7-aryl-3, 9-diazabicyclo(3.3.1)non-6-ene derivatives and their use as renin inhibitors in the treatment of hypertension, cardiovascular or renal diseases

ABSTRACT

The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors or renin.

The invention relates to novel compounds of the general formula I. Theinvention also concerns related aspects including processes for thepreparation of the compounds, pharmaceutical compositions containing oneor more compounds of formula I and especially their use as renininhibitors in cardiovascular events and renal insufficiency.Furthermore, these compounds can be regarded as inhibitors of otheraspartyl proteases and might therefore be useful as inhibitors ofplasmepsins to treat malaria and as inhibitors of Candida albicanssecreted aspartyl proteases to treat fungal infections.

In the renin-angiotensin system (RAS) the biologically activeangiotensin II (Ang II) is generated by a two-step mechanism. The highlyspecific enzyme renin cleaves angiotensinogen to angiotensin I (Ang I),which is then further processed to Ang II by the less specificangiotensin-converting enzyme (acE). Ang II is known to work on at leasttwo receptor subtypes called AT₁ and AT₂. Whereas AT₁ seems to transmitmost of the known functions of Ang II, the role of AT₂ is still unknown.

Modulation of the RAS represents a major advance in the treatment ofcardiovascular diseases. ACE inhibitors and AT₁ blockers have beenaccepted to treat hypertension (Waeber B. et al., “The renin-angiotensinsystem: role in experimental and human hypertension”, in Berkenhager W.H., Reid J. L. (eds): Hypertension, Amsterdam, Elsevier SciencePublishing Co, 1996, 489-519; Weber M. A., Am. J. Hypertens., 1992, 5,247S). In addition, acE inhibitors are used for renal protection(Rosenberg M. E. et al., Kidney International, 1994, 45, 403; Breyer J.A. et al., Kidney International, 1994, 45, S156), in the prevention ofcongestive heart failure (Vaughan D. E. et al., Cardiovasc. Res., 1994,28, 159; Fouad-Tarazi F. et al., Am. J. Med., 1988, 84 (Suppl. 3A), 83)and myocardial infarction (Pfeffer M. A. et al, N. Engl. J. Med., 1992,327, 669).

The rationale to develop renin inhibitors is the specificity of renin(Kleinert H. D., Cardiovasc. Drugs, 1995, 9, 645). The only substrateknown for renin is angiotensinogen, which can only be processed (underphysiological conditions) by renin. In contrast, acE can also cleavebradykinin besides Ang I and can be by-passed by chymase, a serineprotease (Husain A., J Hypertens., 1993, 11, 1155). In patientsinhibition of acE thus leads to bradykinin accumulation causing cough(5-20%) and potentially life-threatening angioneurotic edema (0.1-0.2%)(Israili Z. H. et al., Annals of Internal Medicine, 1992, 117, 234).Chymase is not inhibited by acE inhibitors. Therefore, the formation ofAng II is still possible in patients treated with acE inhibitors.Blockade of the AT₁ receptor (e.g. by losartan) on the other handoverexposes other AT-receptor subtypes to Ang II, whose concentration isdramatically increased by the blockade of AT₁ receptors. This may raiseserious questions regarding the safety and efficacy profile of AT₁receptor antagonists. In summary, renin inhibitors are not only expectedto be different from acE inhibitors and AT₁ blockers with regard tosafety, but more importantly also with regard to their efficacy to blockthe RAS.

Only limited clinical experience (Azizi M. et al., J. Hypertens., 1994,12, 419; Neutel J. M. et al., Am. Heart, 1991, 122, 1094) has beencreated with renin inhibitors because of their insufficient oralactivity due to their peptidomimetic character (Kleinert H. D.,Cardiovasc. Drugs, 1995, 9, 645). The clinical development of severalcompounds has been stopped because of this problem together with thehigh cost of goods. Only one compound containing four chiral centers hasentered clinical trials (Rahuel J. et al., Chem. Biol., 2000, 7, 493;Mealy N. E., Drugs of the Future, 2001, 26, 1139). Thus, metabolicallystable, orally bioavailable and sufficiently soluble renin inhibitorsthat can be prepared on a large scale are missing and sought. Recently,the first non-peptide renin inhibitors were described which show high invitro activity (Oefaer C. et al., Chem. Biol., 1999, 6, 127; PatentApplication WO97/09311; Marki H. P. et al, Il Farmaco, 2001, 56, 21).However, the development status of these compounds is not known.

The present invention relates to the identification of renin inhibitorsof a non-peptidic nature and of low molecular weight. Orally activerenin inhibitors of long duration of action which are active inindications beyond blood pressure regulation where the tissularrenin-chymase system may be activated leading to pathophysiologicallyaltered local functions such as renal, cardiac and vascular remodeling,atherosclerosis, and possibly restenosis are described.

The present invention describes non-peptidic renin inhibitors.

In particular, the present invention relates to novel compounds of thegeneral formula I,

wherein

X and W represent independently a nitrogen atom or a —CH— group;

V represents —(CH₂)_(r)—; -A-(CH₂)_(s)—; —CH₂-A-(CH₂)_(t)—;—(CH₂)_(s)-A-; —(CH₂)₂-A-(CH₂)_(u)—; -A-(CH₂)_(v)—B—;—CH₂—CH₂—CH₂-A-CH₂—; -A-CH₂—CH₂—B—CH₂—; —CH₂-A-CH₂—CH₂—B—;—CH₂—CH₂—CH₂-A-CH₂—CH₂—; —CH₂—CH₂—CH₂—CH₂-A-CH₂—; -A-CH₂—CH₂—B—CH₂—CH₂—;—CH₂-A-CH₂—CH₂—B—CH₂—; —CH₂-A-CH₂—CH₂—CH₂—B—; or —CH₂—CH₂-A-CH₂—CH₂—B—;

A and B independently represent —O—; —S—; —SO—; —SO₂—;

U represents aryl; heteroaryl;

T represents —CONR¹—; —(CH₂)_(p)OCO—; —(CH₂)_(p)N(R¹)CO—;—(CH₂)_(p)N(R¹)SO₂—; or —COO—;

Q represents lower allylene; lower alkenylene;

M represents hydrogen; cycloalkyl; aryl; heterocyclyl; heteroaryl;

L represents —R³; —COR³; —COOR³; —CONR²R³; —SO₂R³; —SO₂NR²R³;—COCH(Aryl)₂;

R¹ represents hydrogen; lower alkyl; lower alkenyl; lower alkinyl;cycloalkyl; aryl; cycloalkyl-lower alkyl;

R² and R²′ independently represent hydrogen; lower alkyl; lower alkenyl;cycloalkyl; cycloalkyl-lower alkyl;

R³ represents hydrogen; lower alkyl; lower alkenyl; cycloalkyl; aryl;heteroaryl; heterocyclyl; cycloalkyl-lower alkyl; aryl-lower alkyl;heteroaryl-lower allyl; heterocyclyl-lower alkyl; aryloxy-lower alkyl;heteroaryloxy-lower alkyl, whereby these groups may be unsubstituted ormono-, di- or trisubstituted with hydroxy, —OCOR², —COOR², lower alkoxy,cyano, —CONR²R²′, CO-morpholin-4-yl, CO-((4-loweralkyl)piperazin-1-yl),—NH(NH)NH², —NR⁴R⁴′ or lower alkyl, with the proviso that a carbon atomis attached at the most to one heteroatom in case this carbon atom issp3-hybridized;

R⁴ and R⁴′ independently represent hydrogen; lower alkyl; cycloalkyl;cycloalkyl-lower alkyl; hydroxy-lower alkyl; —COOR²; —CONH₂;

m and n represent the integer 0 or 1, with the proviso that in case mrepresents the integer 1, n is the integer 0, and in case n representsthe integer 1, m is the integer 0;

p is the integer 1, 2, 3 or 4;

r is the integer 3, 4, 5, or 6;

s is the integer 2, 3, 4, or 5;

t is the integer 1, 2, 3, or 4;

u is the integer 1, 2, or 3;

v is the integer 2, 3, or 4;

and optically pure enantiomers, mixtures of enantiomers such asracemates, diastereomers, mixtures of diastereomers, diastereomericracemates, mixtures of diastereomeric racemates, and the meso-form; aswell as pharmaceutically acceptable salts, solvent complexes andmorphological forms.

In the definitions of general formula I—if not otherwise stated—the termlower alkyl, alone or in combination with other groups, means saturated,straight and branched chain groups with one to seven carbon atoms,preferably one to four carbon atoms that can be optionally substitutedby halogens. Examples of lower alkyl groups are methyl, ethyl, n-propyl,iso-propyl, n-butyl, iso-butyl, sec-butyl, tert-butyl, pentyl, hexyl andheptyl. The methyl, ethyl and isopropyl groups are preferred.

The term lower alkoxy refers to a R—O group, wherein R is a lower alkyl.Examples of lower alkoxy groups are methoxy, ethoxy, propoxy,iso-propoxy, iso-butoxy, sec-butoxy and tert-butoxy.

The term lower alkenyl, alone or in combination with other groups, meansstraight and branched chain groups comprising an olefinic bond andconsisting of two to seven carbon atoms, preferably two to four carbonatoms, that can be optionally substituted by halogens. Examples of loweralkenyl are vinyl, propenyl or butenyl.

The term lower alkinyl, alone or in combination with other groups, meansstraight and branched chain groups comprising a triple bond andconsisting of two to seven carbon atoms, preferably two to four carbonatoms, that can be optionally substituted by halogens. Examples of loweralkinyl are ethinyl, propinyl or butinyl.

The term lower alkylene, alone or in combination with other groups,means straight and branched divalent chain groups with one to sevencarbon atoms, preferably one to four carbon atoms, that can beoptionally substituted by halogens. Examples of lower alkylene areethylene, propylene or butylene.

The term lower alkenylene, alone or in combination with other groups,means straight and branched divalent chain groups comprising an olefinicbond and consisting of two to seven carbon atoms, preferably two to fourcarbon atoms, that can be optionally substituted by halogens. Examplesof lower alkenylene are vinylene, propenylene and butenylene.

The term lower alkylenedioxy, refers to a lower alkylene substituted ateach end by an oxygen atom. Examples of lower alkylenedioxy groups arepreferably methylenedioxy and ethylenedioxy.

The term lower alkylenoxy refers to a lower alkylene substituted at oneend by an oxygen atom. Examples of lower alkylenoxy groups arepreferably methylenoxy, ethylenoxy and propylenoxy.

The term halogen means fluorine, chlorine, bromine or iodine, preferablyfluorine, chlorine and bromine.

The term cycloalkyl alone or in combination, means a saturated cyclichydrocarbon ring system with 3 to 7 carbon atoms, e.g. cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, which can beoptionally mono- or multisubstituted by lower alkyl, lower alkenyl,lower alkenylene, lower alkoxy, lower alkylenoxy, lower alkylenedioxy,hydroxy, halogen, —CF₃, —NR¹R¹′, —NR¹C(O)R¹′, —NR¹S(O₂)R¹′, —C(O)NR¹R¹′,lower alkylcarbonyl, —COOR¹, —SR¹, —SOR¹, —SO₂R¹, —SO₂NR¹R¹′ whereby R¹′represents hydrogen; lower alkyl; lower alkenyl; lower alkinyl;cycloalkyl; aryl; cycloalkyl-lower alkyl. The cyclopropyl group is apreferred group.

The term aryl, alone or in combination, relates to the phenyl, thenaphthyl or the indanyl group, preferably the phenyl group, which can beoptionally mono- or multisubstituted by lower alkyl, lower alkenyl,lower alkinyl, lower alkenylene or lower alkylene forming with the arylring a five- or six-membered ring, lower alkoxy, lower alkylenedioxy,lower alkylenoxy, hydroxy, hydroxy-lower alkyl, halogen, cyano, —CF₃,—OCF₃, —NR¹R¹, —NR¹R¹-lower alkyl, —NR¹C(O)R¹′, —NR₁S(O₂)R¹,—C(O)NR¹R¹′, —NO₂, lower alkylcarbonyl, —COOR¹, —SR¹, —SOR¹, —SO₂R¹,—SO₂NR¹R¹′, benzyloxy, whereby R¹′ has the meaning given above.Preferred substituents are halogen, lower alkoxy, lower alkyl, CF₃,OCF₃.

The term aryloxy refers to an Ar—O group, wherein Ar is an aryl. Anexample of a lower aryloxy group is phenoxy.

The term heterocyclyl, alone or in combination, means saturated orunsaturated (but not aromatic) five-, six- or seven-membered ringscontaining one or two nitrogen, oxygen or sulfur atoms which may be thesame or different and which rings can be optionally substituted withlower alkyl, hydroxy, lower alkoxy and halogen. The nitrogen atoms, ifpresent, can be substituted by a —COOR² group. Examples of such ringsare piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl,tetrahydropyranyl, dihydropyranyl, 1,4-dioxanyl, pyrrolidinyl,tetrahydrofuranyl, dihydropyrrolyl, imidazolidinyl, dihydropyrazolyl,pyrazolidinyl, dihydroquinolinyl, tetrahydroquinolinyl,tetrahydroisoquinolinyl.

The term heteroaryl, alone or in combination, means six-memberedaromatic rings containing one to four nitrogen atoms; benzofusedsix-membered aromatic rings containing one to three nitrogen atoms;five-membered aromatic rings containing one oxygen, one nitrogen or onesulfur atom; benzofused five-membered aromatic rings containing oneoxygen, one nitrogen or one sulfur atom; five-membered aromatic ringscontaining one oxygen and one nitrogen atom and benzofused derivativesthereof; five-membered aromatic rings containing a sulfur and a nitrogenor an oxygen atom and benzofused derivatives thereof; five-memberedaromatic rings containing two nitrogen atoms and benzofused derivativesthereof; five-membered aromatic rings containing three nitrogen atomsand benzofused derivatives thereof, or a tetrazolyl ring. Examples ofsuch ring systems are furanyl, thiophenyl, pyrrolyl, pyridinyl,pyrimidinyl, indolyl, quinolinyl, isoquinolinyl, imidazolyl, triazinyl,thiazinyl, thiazolyl, isothiazolyl, pyridazinyl, pyrazolyl, oxazolyl,isoxazolyl, coumarinyl, benzothiophenyl, quinazolinyl, quinoxalinyl.Such rings may be adequately substituted with lower alkyl, loweralkenyl, lower alkinyl, lower alkylene, lower alkenylene, loweralkylenedioxy, lower alkyleneoxy, hydroxy-lower alkyl, lower alkoxy,hydroxy, halogen, cyano, —CF₃, —OCF₃, —NR¹R¹′, —NR¹R¹′-lower alkyl,—N(R¹)COR¹, —N(R¹)SO₂R¹, —CONR¹R¹′, —NO₂, lower alkylcarbonyl, —COOR¹,—SR¹, —SOR¹, —SO₂R¹, —SO₂NR¹R¹′, another aryl, another heteroaryl oranother heterocyclyl and the like, whereby R¹′ has the meaning givenabove.

The term heteroaryloxy refers to a Het-O group, wherein Het is aheteroaryl.

The term sp3-hybridized refers to a carbon atom and means that thiscarbon atom forms four bonds to four substituents placed in a tetragonalfashion around this carbon atom.

The expression pharmaceutically acceptable salts encompasses eithersalts with inorganic acids or organic acids like hydrochloric orhydrobromic acid, sulfuric acid, phosphoric acid, citric acid, formicacid, acetic acid, maleic acid, tartaric acid, benzoic acid,methanesulfonic acid, p-toluenesulfonic acid, and the like that are nontoxic to living organisms or in case the compound of formula I is acidicin nature with an inorganic base like an alkali or earth alkali base,e.g. sodium hydroxide, potassium hydroxide, calcium hydroxide and thelike.

The compounds of the general formula I can contain two or moreasymmetric carbon atoms and may be prepared in form of optically pureenantiomers, mixtures of enantiomers such as racemates, diastereomers,mixtures of diastereomers, diastereomeric racemates, mixtures ofdiastereomeric racemates, and the meso-form and pharmaceuticallyacceptable salts thereof.

The present invention encompasses all these forms. Mixtures may beseparated in a manner known per se, i.e. by column chromatography, thinlayer chromatography, HPLC or crystallization.

A group of preferred compounds are compounds of general formula Iwherein X, W, V, U, T, Q, L, and M are as defined in general formula Iabove and wherein

n is 0 and

m is 1.

Another group of preferred compounds of general formula I are thosewherein X, W, V, U, T, Q, M, m, and n are as defined in general formulaI above and

L represents H; —COR³″; —COOR³″; —CONR²″R³″;

whereby R²″ and R³″ represent independently lower alkyl, lowercycloalkyl-lower alkyl, which lower alkyl and lower cycloalkyl-loweralkyl groups are unsubstituted or monosubstituted with halogen, cyano,hydroxy, —OCOCH₃, —CONH₂, —COOH, —NH₂, with the proviso that a carbonatom is attached at the most to one heteroatom in case this carbon atomis sp3-hybridized.

Another group of preferred compounds of general formula I above arethose wherein X, W, V, U, L, m, and n are as defined in general formulaI and

T is —CONR¹;

Q is methylene;

M is hydrogen; aryl; or heteroaryl.

Another group of even more preferred compounds of general formula I arethose wherein X, W, U, L, T, Q, M, m, and n are as defined in generalformula I above and

V is —CH₂CH₂O—; —CH₂CH₂CH₂O—; —OCH₂CH₂O—; —

Another group of also more preferred compounds of general formula I arethose wherein V, U, T, Q, M, L, m, and n are as defined in generalformula I above and X and W represent —CH—.

Another group of also more preferred compounds of general formula I arethose wherein X, W, V, Q, T, M, L, m, and n are as defined in generalformula I above and

U is a mono-, di-, or trisubstituted phenyl wherein the substituents arehalogen; lower alkyl or lower alkoxy.

Especially preferred compounds of general formula I are those selectedfrom the group consisting of:

-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-5-methylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-bromo-3-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-phenoxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,4-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(4-bromo-3-methylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-acetylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-ethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3,5-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3,4-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-[4-(3-o-tolyloxypropyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{6-[3-(2-methoxy-benzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-en-6-yliethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-Acetyl-7-[4-(2-m-tolyloxyethyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3-methoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-3-trifluoromethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-tert-butyl-2-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[3-(2-bromophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-isopropylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3-bromophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromophenoxy)propyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-[4-(3-o-tolyloxy-propyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3,4-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-tert-butylphenoxy)propyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3-chlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-ethylphenoxy)propyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3-trifluoromethoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3,4-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-4,5-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chlorophenyl)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   5 (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-[2-(4-chlorophenyl)ethyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-yl    methyl ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-3-trifluoromethylphenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethyl-amide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[2-(3-chloro-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-[4-(2-tolyloxyethoxy)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,4-dichlorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,5-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-ethoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[3-(3-chlorophen-oxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3,5-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[2-(2-chlorophen-oxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,5-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,5-trimethylphenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3-chlorophenyl)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,6-trifluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[3-(2-trifluoro-methylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3-trifluoromethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide,-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3,5-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(m-tolyloxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-methoxyphenyl)ethoxy]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(4-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3,4-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[3-(3-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid phenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-[4-(3-phenoxypropyl)-phenyl]-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-acetyl-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-6-[2-(2-methoxyphenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-tert-butylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-propionylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   1:1 mixture of (2R)— and    (2S)—N-((1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyl-oxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl)-N-methyl-2-phenylpropionamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-tert-butyl-4-methylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-tert-butyl-6-methylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(4-chloro-2-methoxyphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-methoxy-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3-methoxyphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   5    (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(4-tert-butyl-2-methylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3,5-dimethoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-iso-propylphenoxy)ethyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-methoxyphenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3-bromophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-[4-(3-p-tolyloxypropyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-acetic acid    2-((1R*,5S*)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]methylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2-oxoethyl    ester;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3-(2-cyanoacetyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]-methylamide;-   (rac.)-(1R*,5S*)-3-(2-acetylaminoacetyl)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)-ethyl]methylamide;-   1:1 mixture of    (1R,5S)-3-((4R)-2-acetylamino-4-methylpentanoyl)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]methylamide and    (1S,5R)-3-((4R)-2-acetylamino-4-methylpentanoyl)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-hydroxybenzyl)methylamide;-   1:1 mixture of    (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [(3R*)-3-(2-chloro-phenyl)butyl]methylamide and    (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophen-oxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [(3S*)-3-(2-chlorophenyl)butyl]methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methyl-(4-phenylbutyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methyl-(3-phenoxypropyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methyl-(4-phenylpentyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-benzo[1,3]dioxol-5-ylpropyl)methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(4-methoxyphenoxy)ethyl]methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(4-chlorophenoxy)ethyl]methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methyl-(2-p-tolyloxyethyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid diethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methyl-(2-pyridin-2-ylethyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(4-methoxyphenoxy)ethyl]methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methyl-(3-trifluoromethylbenzyl)-amide;-   (rac.)—(R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(3,4-dimethylphenoxy)ethyl]methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3,5-dimethoxybenzyl)methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3,4-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)isopropylamide;-   (rac.)-(1R*,5S*)-5-[7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxo-pentanoic    acid;-   (1S,5R)-3-acetyl-7-{4-[2-(2,3,6-trifluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   1:1-mixture of    (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-((2R*)-2,3-dihydroxypropyl)benzyl]amide and    (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-((2S*)-2,3-dihydroxypropyl)benzyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxy-ethyl)benzyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylcyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methyl-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-m-tolyloxy-ethyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(3,4-dimethyl-phenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-fluoro-phenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-o-tolylethyl)-amide;-   1:1-mixture of    (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid ((2R*)-2-hydroxy-2-phenylethyl)methylamide and    (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid ((2S*)-2-hydroxy-2-phenylethyl)methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoro-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-o-tolylethyl)-amide;-   (rac.)-(1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-(1R*,5S*)-6-[(2-fluorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-(1R*,5S*)-6-[(2-methylbenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-(1R*,5S*)-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-(1R*,5S*)-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-(1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(3-methoxyphenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-m-tolyloxyethyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamnoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-fluorophenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-o-tolylethyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)amide;-   1:1-mixture of    (1R*,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylcyclopropylamide and    (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylcyclopropylamide;-   1:1-mixture of    (1R*,5S*)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide and    (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   1:1-mixture of    (1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide and    (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   1:1-mixture of    (1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethylbenzyl)amide and (1S,5R)-3-((1S,    4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethylbenzyl)amide;-   1:1-mixture of    (1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide and    (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methyl-enzyl)amide;-   1:1-mixture of    (1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-m-tolyloxyethyl)amide and    (1S,5R)-3-((1R,4S-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-in-tolyloxy-ethyl)amide;-   1:1-mixture of    (1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide and (1S,5R)-3-((1S,    4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   1:1-mixture of    (1R,5S)-3-((1S,4R)-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)amide and    (1S,5R)-3-((1S,4R)-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)-amide;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxy-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3,4-dimethyl-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-(6-(cyclopropylphenethyl-carbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-5-(6-(cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-(1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-o-tolylethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-((1R*,    5S*)-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-(1R*,5S*)-6-[cyclopropyl-(2-p-tolylethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3R*)-5-((1R*,    5S*)-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylcyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(3-methoxy-phenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(3-methyl-phenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl(2-p-tolylethyl)amide;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-(cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylmethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-(cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-(cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[(2-chlorobenzyl)ethyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethyl-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and (rac.)-(2S*,    3R*)-4-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2-methyl-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxy-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and (rac.)-(2S*,    3R*)-4-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(4-methyl-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-(1R*,5S*)-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-((1R*,    5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-[4-[3-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid methyl ester;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)-benzyl]amide;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-(4-carbanoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-2,2-dimethyl-5-oxopentalioic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chloro-benzyl)ethylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid and (rac.)-(2S*,    3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]-phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid and (rac.)-(2S*,    3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid; 1:1-mixture of    (rac.)-(2R*,3S*)-4-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl]-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropyl-phenethylcarbamoyl)-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl]-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)ethylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide;-   (rac.)—(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2,3-difluorophenyl)ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(4-fluorophenyl)ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-methylphenyl)ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(4-methylphenyl)ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)ethyl-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-{(1R*,    5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3R*)-5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethyl-carbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluoro-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methyl-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methyl-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanioic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)-benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-fluorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-trifluoromethylbenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-methylbenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]amide;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{(2-chlorobenzyl)ethylcarbamoyl}-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-(2-fluorobenzyl)cyclopropylcarbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanioic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-(1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid methyl ester;-   (rac.)-5-((1R*,    S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and (rac.)-(3S*)-4-((1R*,    5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzyl-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   1:1-mixture of    (1R,5S)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide and    (1S,5R)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   1:1-mixture of    (rac.)-(3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid and (rac.)-(3S*)-4-{(1R*,    5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)-cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzyl-cyclopropylamide;-   1:1-mixture of    (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid and    (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)-methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester and    (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   1:1-mixture of    (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid and    (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid ((2R*)-2-hydroxy-2-phenylethyl)methylamide and    (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid ((2R*)-2-hydroxy-2-phenylethyl)-methylamide;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-{(1R*,    5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)-cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]-cyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(p-toluoyl-ethyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)-amide;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[(2-chloro-benzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[2-(4-bromophenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoic    acid;-   (rac.)-5-{[(R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylcyclopropyl-amide;-   (rac.)-(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-ethylamide;-   (rac.)-(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)-ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)—(R*,5S*)-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide;-   (rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-formyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-ethylamide;-   (rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-formyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-o-tolylethyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-formyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)amide;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-{(R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-[(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-[(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-[(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamnoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylcyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamnoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropylphenethylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-fluorophenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-o-tolylethyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxo-pentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-drimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-6-[cyclopropyl-(3-trifluormethylobenzyl)carbamoyl]-3,9-diazabicycl-o[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-[(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl]-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-[(1R*,    5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropyl-phenethylcarbamoyl)-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl]-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (1R,5S)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide and    (1S,5R)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   1:1-mixture of    (1R,5S)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide and    (1S,5R)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)-benzyl]amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide;-   (rac.)-5-((1R*,5S*)-6-(cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-(1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-(1R*,5S*)-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   1:1-mixture of    (rac.)-5-((1R*,5S*)-6-[cyclopropyl-((2R*)-2-hydroxy-2-phenylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid and    (rac.)-5-((1R*,5S*)-6-[cyclopropyl-((2S*)-2-hydroxy-2-phenylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,    S*)-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   25    (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-phenethylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chloro-phenyl)-ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-fluorophenyl)ethyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide;-   (rac.)-acetic acid    (1R*,5S*)-2-(2-{[(3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy-)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbonyl)cyclopropylamino]-methyl}phenyl)ethyl    ester;-   (rac.)-acetic acid    (1R*,5S*)-2-(2-{[(3-acetyl-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbonyl)-cyclopropylamino]methyl}phenyl)ethyl    ester;-   (rac.)-(1R*,5S*)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-fluorophenyl)ethyl]-amide;-   (rac.)-(1R*,5S*)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)-amide;-   (rac.)-acetic acid    (1R*,5S*)-2-(2-{[(3-acetyl-7-{4-[2-(4-bromophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbonyl)cyclopropylamino]methyl}-phenyl)ethyl    ester;-   1:1 mixture of    (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid and    (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylcyclopropylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethylbenzyl)-amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxyphenoxy)-ethyl]amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]cyclopropyl-amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(2,3-difluorophenyl)-ethyl]amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-o-tolylethyl)amide;-   (rac.)—(R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-p-tolylethyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,5-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(3-cyanopyridin-2-yloxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,5-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3,5-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,6-trichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methoxybenzyl)-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(5-fluoro-2-methoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,6-difluoro-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-fluoro-2-methyl-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3,6-difluorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-difluoro-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(4-fluorobenzyl)-amide;-   (rac.)—(R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)-amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-[2-(4-methoxyphenoxy)-ethyl]amide;-   (rac.)-(1R*,5S*)-3-methyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-ethyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-(2-aminoacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(3-aminopropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoro-methylbenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethyl-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoromethyl-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichlorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (6-chloro-benzo[1,3]dioxol-5-ylmethyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoromethylbenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy-ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-difluorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,4-dimethoxybenzyl)amide;-   (rac.)—(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (6-chloro-benzo[1,3]-dioxol-5-ylmethyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,4-dimethoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methyl-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-difluorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,4-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethoxybenzoyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methyl-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (6-chloro-benzo[1,3]dioxol-5-ylmethyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,6-dichloro-4-methylphenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide formate salt;-   (rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide.

Most preferred compounds of general formula I are those selected fromthe group consisting of

-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-(2-thiophen-2-ylacetyl)-3,9-diazabicyclo[3.3.1]non-6-en-6-yl-methyl    ester;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-(quinoxaline-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chlorophenyl)ethyl]methyl-amide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-(benzo[b]thiophene-3-carbonyl)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-6-yl-methyl    ester;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxy-benzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-phenylmethanesulfonyl-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(4-methoxyphenyl)ethyl]-methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{6-[3-(2-methoxybenzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(4-chlorophenyl)ethyl]methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(3-chlorophenyl)ethyl]methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid ethylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(3-methoxyphenyl)ethyl]methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-methyl-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(3,4-dimethoxyphenyl)ethyl]-methylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,5-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-N-((1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(2-methoxyphenyl)acetic acid    (1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl    ester;-   (rac.)-N-((1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl)-2-(2-methoxyphenyl)-N-methyl-acetamide;-   (rac.)-N-((1R*,5S*)-3-acetyl-7-{4-[2-(2-tert-butyl-4-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,5-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo    [3.3.1]non-6-ene-6-carboxylic acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methyl(3-phenylpropyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-acetylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-methoxyphenyl)ethyl]methyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzylmethylamine;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,5-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-[4-(2-o-tolyloxyethyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(3-isopropylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid methylphenethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-5-[7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophonoxy)propyl-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-(1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid 2,2,2-trichloro-1,1-dimethylethyl ester;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid methyl ester;-   1:1-mixture of    (1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide and    (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzyl-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-phenethylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid [2-(2-chloro-phenyl)ethyl]cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-((1R*,    5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazbicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-((1R*,    S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazbicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethyl-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-((1R*,    S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-m-tolyloxyethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and (rac.)-(3S*)-5-((1R*,    S*)-6-[cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]-cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxy-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid and    (rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl(3,5-dimethoxy-benzyl)amide;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-(1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid; 1:1-mixture of    (rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyric    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid methyl ester;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   1:1-mixture of    (rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid and    (rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyric    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(3-trifluoromethylbenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-methylbenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)cyclopropylamide;-   (rac.)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid methyl ester;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,    S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-(1R*,5S*)-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-(cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)ethylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylic    acid 6-[(2-chlorobenzyl)cyclopropyl-amide]3-dimethylamide;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylic    acid 6-[(2-chlorobenzyl)cyclopropyl-amide]3-diethylamide;-   (rac.)-(1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic    acid methyl ester;-   (rac.)-(1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic    acid ethyl ester;-   (rac.)-(1R*,5S*)-3-methanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-ethanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoic    acid ethyl ester;-   (rac.)-4-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-4-oxo-butyric    acid;-   (rac.)-3-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)-amino]propionic    acid ethyl ester;-   (rac.)4-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,39,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)-amino]butyric    acid ethyl ester;-   (rac.)-(1R*,5S*)-3-(3-carbamoylpropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(2-hydroxyacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (1S,5R)-3-((3R)-3-hydroxybutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   1:1-mixture of    (rac.)-(1R*,5S*)-3-((1R*,2S*)-2-hydroxycyclopentanecarbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide and    (rac.)-(1R*,5S*)-3-((1S*,2R*)-2-hydroxycyclopentanecarbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-9-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-5-oxo-pentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-5-oxo-pentanoic    acid ethyl ester;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-5-oxo-pentanoic    acid methyl ester;-   1:1-mixture of    (rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-9-yl)-3-hydroxy-5-oxo-pentanoic    acid and (rac.)-(3S*)-5-((1R*,    5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-9-yl)-3-hydroxy-5-oxopentanoic    acid;-   (rac.)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-2,2-dimethyl-5-oxopentanoic    acid;-   (rac.)-4-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-4-oxo-butyric    acid;-   (rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylic    acid 6-[(2-chlorobenzyl)cyclopropyl-amide]9-dimethylamide;-   (rac.)-(1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid methyl ester;-   (rac.)-(1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic    acid ethyl ester;-   (rac.)-3-[(1R*,5S*)-(6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)-amino]propionic    acid ethyl ester;-   (rac.)-4-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)-amino]butyric    acid ethyl ester;-   (rac.)-(1R*,5S*)-3-formyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)-3-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)-amino]propionic    acid;-   (rac.)-3-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)-amino]propionic    acid;-   (rac.)-4-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)-amino]butyric    acid;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,6-trifluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropyl-amide;-   (rac.)—(1R*,5S*)-9-(4-carbamoylbutyryl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-9-(3-carbamoylpropionyl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-9-(2-hydroxyacetyl)-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (1R,5S)-9-((3S)-3-hydroxybutyryl)-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-9-methanesulfonyl-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-9-ethanesulfonyl-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-5-methoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methoxybenzyl)-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,4-dimethoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoromethyl-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid benzo[1,3]dioxol-5-ylmethyl-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-6-fluorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethyl-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-difluoro-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichloro-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethoxy-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methylbenzyl)-amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-chlorobenzyl)cyclopropyl-amide;-   (rac.)-(1R*,5S*)-3-(5-morpholin-4-yl-5-oxopentanoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(2-tetrazol-1-ylacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-(5-oxo-5-piperazin-1-ylpentanoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   1:1-mixture of    (1R,5S)-3-((2S)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide and    (1S,5R)-3-((2S)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   1:1-mixture of    (1R,5S)-3-((2S)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide and    (1S,5R)-3-((2S)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichlorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoromethyl-benzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-ethylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (6-chlorobenzo-[1,3]dioxol-5-ylmethyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,5-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichloro-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoro-methylbenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (3-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-methylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichlorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-3,6-difluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoromethylbenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3,4-dimethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(3-trifluoromethoxybenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-chloro-3-trifluoro-methylbenzyl)cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichlorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethyl-benzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethylbenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichlorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid (2-bromobenzyl)-cyclopropylamide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dichlorobenzyl)amide;-   (rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic    acid cyclopropyl-(2,3-dimethylbenzyl)amide;-   (rac.)-(1R,5S)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide;-   (rac.)-(1S,5R)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylic    acid (2-chlorobenzyl)cyclopropylamide.

The compounds of general formula I and their pharmaceutically acceptablesalts may be used as therapeutics e.g. in form of pharmaceuticalcompositions. They may especially be used in the treatment and/orprophylaxis of cardiovascular and renal diseases. Examples of suchdiseases are hypertension, coronary diseases, cardiac insufficiency,renal insufficiency, renal and myocardial ischemia, and renal failure.They can also be used to prevent restenosis after balloon or stentangioplasty, to treat erectile dysfunction, glomerulonephritis, renalcolic, and glaucoma. Furthermore, they can be used in the therapy andthe prophylaxis of diabetic complications, complications of vascular orcardiac surgery or after organ transplantation, complications ofcyclosporin treatment, as well as other diseases presently known to berelated to the RAS.

In another embodiment, the invention relates to a method for thetreatment and/or prophylaxis of diseases which are related to the RASsuch as hypertension, coronary diseases, cardiac insufficiency, renalinsufficiency, renal and myocardial ischemia, and renal failure, whichmethod comprises administrating a compound as defined above to a humanbeing or animal.

The invention further relates to the use of compounds of general formulaI as defined above for the treatment and/or prophylaxis of diseaseswhich are associated with the RAS such as hypertension, coronarydiseases, cardiac insufficiency, renal insufficiency, renal andmyocardial ischemia, and renal failure.

In addition, the invention relates to the use of compounds as definedabove for the preparation of medicaments for the treatment and/orprophylaxis of diseases which are associated with the RAS such ashypertension, coronary diseases, cardiac insufficiency, renalinsufficiency, renal and myocardial ischemia, and renal failure.

The compounds of formula I may also be used in combination with one ormore other therapeutically useful substances e.g. with other renininhibitors, with acE-inhibitors, with angiotensin-receptor antagonists,with diuretics, with calcium channel blockers, with endothelin receptorsantagonists or with other drugs beneficial for the prevention or thetreatment of cardiovascular events or renal insufficiency.

All forms of prodrugs leading to an active component comprised bygeneral formula I above are included in the present invention.

The compounds of general formula I can be manufactured by the methodsoutlined below, by the methods described in the examples or by analogousmethods.

Preparation of the Precursors:

Precursors are compounds which were prepared as key intermediates and/orbuilding blocks and which were suitable for further transformations inparallel chemistry.

Bicyclononanone A was prepared from(4-benzyl-6-ethoxycarbonylmethyl-1-methylpiperazin-2-yl)acetic acidethyl ester (Patent Application WO92/05174) as described in Scheme 1.Derivative A might also be present as enol form. In order to allow acoupling at the 7-position of bicyclononane A with aryl bromides, thevinyl triflate derivative B was prepared.

The bromoaryl components can be prepared as described in Scheme 2. AMitsunobu coupling (→compounds of type C) or the alkylation of analcohol with a benzylic chloride (or bromide, →compounds of type D) areoften the most convenient methods. Derivatives E and F were prepared inone step from 1-(3-chloropropoxymethyl)-2-methoxybenzene (Vieira E. etal., Bioorg. Med. Chem. Letters, 1999, 9, 1397) or3-(5-bromopyridin-2-yloxy)propan-1-ol (Patent Application WO 98/39328)according to these methods. Other methods for the preparation of ethersor thioethers, like a Williamson synthesis, might be used as well (seee.g. March, J, “Advanced Organic Chemistry,”, 3^(rd) ed., John Wiley andsons, 1985).

As shown in Scheme 3, these bromoaryl derivatives might then be coupledto triflate B in the presence of Pd(PPh₃)₄ or a related Pd(0)-complex inorder to obtain bicyclononenes G (for details see the correspondingexamples). Protective group manipulation would lead to thebicyclononenes H, which can finally be reduced to the alcoholderivatives J.

If R^(a) is O-SEM and X is CH, in compounds of type J, theSEM-protecting group can be cleaved under slightly acidic conditions,while the Boc-protecting group remains untouched as illustrated inScheme 4. The phenolic moiety of bicyclononene K might then be alkylatedto bicyclononene L. This alcohol intermediate would be transformed intothe ester M, and the Boc-protecting group can finally be cleaved toyield precursor N.

If X is N (Scheme 3), bicyclononenes of type J can be esterified tobicyclononenes O that can be deprotected to precursors P (Scheme 5).

If, in alkohols J, X is CH (Scheme 6) and, for instance, R^(a) isO(CH₂)_(q)OTBDMS or (CH₂)_(q)OTBDMS (Scheme 3), an esterification mightlead to bicyclononenes Q (Scheme 6). Under acidic conditions, both theBoc- and the TBDMS-groups would be cleaved and the secondary amine mightbe acylated, sulfonated, or alkylated to yield precursors R.

As illustrated in Scheme 7, the Boc-protecting group of bicyclononenes Hmight be cleaved and the resulting secondary amine acylated, sulfonated,or N-alkylated to bicyclononenes S. Saponification of the ester wouldlead to precursors T. If, for instance, R^(a) is O(CH₂)_(n)OTBDMS or(CH₂)_(n)OTBDMS, the silyl ether might be cleaved simultaneously duringthe cleavage of the Boc-protecting group or during the saponification.The acid might be transformed into an amide to lead to precursors U.Alternatively, amides U can be prepared from bicyclononenes H throughthe acids V, with simultaneous cleavage of the silyl ether. Reaction ofthe acids V with amines might give the amides W that can be transformedinto precursors U. The amines can be prepared according to theliterature or as described in the experimental part.

As illustrated in Scheme 8, the bicyclononenes S might be reduced to thecorresponding alcohols X. The alcohol derivative X might then beoxidised to the aldehydes Y, which might transformed to the precursors Zby reductive amination.

As shown in Scheme 9, a compound of type H might also be saponified to acompound of type AA. After amide coupling to a derivative of type AB,removal of the Boc-group would yield a precursor of type ac.

As illustrated in Scheme 10, a compound of type S might also betransformed into a compound of type AH that in turn can be saponified toa precursor of type AJ.

Alternatively precursors of type AJ might be prepared frombicyclononanone A, but using the benzyl ester instead of the ethylester, as illustrated in Scheme 11. After a transesterification tocompound AM similar reactions as described here above would lead tocompounds AN, AO, AP, AQ, AR and finally AJ.

As shown in Scheme 12 a precursor of type AL might be prepared as wellin two steps from a compound of type W.

Sometimes it might be necessary to transform a substituent further afterattaching it on the bicyclic template. For instance a compound of typeAS, obtained by amide coupling from a compound of type AJ, might betransformed into a precursor of type AT, AU, or AV, as illustrated inScheme 13.

As illustrated in Scheme 14 compounds of type H might be deprotectedinto compounds of type AW. This type of compounds might be thentransformed into compounds of type AX and finally into compounds of typeAY. Compounds of type AY might also be prepared from compounds of typeAP. Compounds of type AY might be transformed into compounds of type AK.Compounds of type AK might be finally transformed into precurosrs oftype AL.

Alternatively, as shown in Scheme 15, AX might be transformed into acompound of type BL, than might be then lead to a compound of type AJ.

As shown in Scheme 16 compounds of type H or S might be transformed intocompounds of type AZ (the substituent at the N(3) position be L or Boc).Then compounds of type T might be obtained that might be thentransformed into compounds of type BA. Finally precursors of type BBmight be prepared.

Also, as shown in Scheme 17, compounds of type AK might be transformedinto precursors of type BC.

Also, a compound of type S might be transformed into a compound of typeBM, as shown in Scheme 18. A compound of type BM might be thensaponified not a precursor of type BN.

Preparation of the Secondary Amines

It might be necessary to prepare secondary amines as well. This might bedone by reductive amination from the corresponding amine and aldehyde,or by amide coupling, from the corresponding amine and carboxylic acid,followed by reduction with LAH or borane. These standard procedures arewell-described in the literature. (2-Allylphenyl)cyclopropylamine,necessary for instance in Scheme 13, might be prepared by allylation of2-bromobenzaldehyde, protected as an acetal; subsequent deprotection tothe 2-allylbenzaldehyde and reductive amination would lead to thedesired amine.

Preparation of Final Compounds

From precursors prepared as described above, the final compounds can beprepared using parallel chemistry techniques. For the specific examples,see the experimental part.

Diazabicyclononenes of type of N can be acylated, or alkylated, orsulfonated, using standard procedures (Scheme 19), and then directlydeprotected to yield the final compounds (for numbering, see specificexamples). In each case, purification by preparative HPLC might give thecorresponding TFA salts or formate salts.

Precursors R, U or BB (with a L-substituent at the N(3)-position) mightbe transformed into the corresponding aryl ethers (Scheme 20), using theMitsunobu reaction conditions. After deprotection, the final compoundsare obtained.

Precursors T, AJ or AV might be submitted to an amide coupling (Scheme21). Deprotection would lead to the desired final compounds.

Compounds Z might be reacted with acylating (or sulfonating) reagents tolead to the corresponding amides (or sulfonamides) as well (Scheme 22).Deprotection would lead to the final compounds.

Compounds of type ac or AL can be reacted as well with acylating,sulfonating or alkylating reagents (Scheme 23). After deprotection, thefinal compounds would be obtained.

Precursors of type BC might also lead to final compounds as indicated inScheme 24.

Enantioselective Synthesis:

The compounds of the present invention contain at least two chiralcenters which, however, are not independent from each other. Thesynthetic methods presented so far might lead to racemates. Bothenantiomers might be prepared selectively starting from ameso-bicyclononane derivative, like compound AD (Blount B. K., Robinson,R., J. Chem. Soc., 1932, 2485) or AE, prepared similarly to compound Awith a subsequent decarboxylation (Scheme 25). For instance, compound AEmight be stereoselectively acylated to bicyclononane derivatives AF orAG as already described elsewhere for similar compounds (Majewski M.,Lasny R., J. Org. Chem., 1995, 60, 5825). Similarly, the otherenantiomer might be prepared.

Finally precursor BK might be prepared as described in Scheme 26.

The compounds of formula I and their pharmaceutically acceptable acidaddition salts can be used as medicaments, e.g. in the form ofpharmaceutical preparations for enteral, parenteral, or topicaladministration. They can be administered, for example, perorally, e.g.in the form of tablets, coated tablets, dragées, hard and soft gelatinecapsules, solutions, emulsions or suspensions, rectally, e.g. in theform of suppositories, parenterally, e.g. in the form of injectionsolutions or infusion solutions, or topically, e.g. in the form ofointments, creams or oils. The production of pharmaceutical preparationscan be effected in a manner which will be familiar to any person skilledin the art by bringing the described compounds of formula I and theirpharmaceutically acceptable acid addition salts, optionally incombination with other therapeutically valuable substances, into agalenical administration form together with suitable, non-toxic, inert,therapeutically compatible solid or liquid carrier materials and, ifdesired, usual pharmaceutical adjuvants.

Suitable carrier materials are not only inorganic carrier materials, butalso organic carrier materials. Thus, for example, lactose, corn starchor derivatives thereof, talc, stearic acid or its salts can be used ascarrier materials for tablets, coated tablets, dragées and hard gelatinecapsules. Suitable carrier materials for soft gelatine capsules are, forexample, vegetable oils, waxes, fats and semi-solid and liquid poyols(depending on the nature of the active ingredient no carriers are,however, required in the case of soft gelatine capsules). Suitablecarrier materials for the production of solutions and syrups are, forexample, water, polyols, sucrose, invert sugar and the like. Suitablecarrier materials for injections are, for example, water, alcohols,polyols, glycerols and vegetable oils. Suitable carrier materials forsuppositories are, for example, natural or hardened oils, waxes, fatsand semi-liquid or liquid polyols. Suitable carrier materials fortopical preparations are glycerides, semi-synthetic and syntheticglycerides, hydrogenated oils, liquid waxes, liquid paraffins, liquidfatty alcohols, sterols, polyethylene glycols and cellulose derivatives.

Usual stabilizers, preservatives, wetting and emulsifying agents,consistency-improving agents, flavour-improving agents, salts forvarying the osmotic pressure, buffer substances, solubilizers, colorantsand masking agents and antioxidants come into consideration aspharmaceutical adjuvants.

The dosage of compounds of formula I can vary within wide limitsdepending on the disease to be controlled, the age and the individualcondition of the patient and the mode of administration, and will, ofcourse, be fitted to the individual requirements in each particularcase. For adult patients a daily dosage of about 1 mg to about 1000 mg,especially about 50 mg to about 500 mg, comes into consideration.

The pharmaceutical preparations conveniently contain about 1-500 mg,preferably 5-200 mg of a compound of formula I.

The following examples serve to illustrate the present invention in moredetail. They are, however, not intended to limit its scope in anymanner.

EXAMPLES General Remarks

The compounds were characterized at least by LC-MS and ¹H-NMR. Only theLC-MS data are given here.

ABBREVIATIONS

AcCl Acetyl chloride

acE Angiotensin Converting Enzyme

AcOH Acetic acid

Ang Angiotensin

aq. aqueous

9-BBN 9-Borabicyclo[3.3.1]nonane

Bn Benzyl

Boc tert-Butyloxycarbonyl

BSA Bovine serum albumine

BuLi n-Butyllithium

CDI 1,1-Carbonyldiimidazol

conc. concentrated

DIBAL Diisobutylaluminium hydride

DIPEA Diisopropylethylamine

DMAP 4-N,N-Dimethylaminopyridine

DMF N,N-Dimethylformamide

DMSO Dimethylsulfoxide

EDC HCl Ethyl-N,N-dimethylaminopropylcarbodiimide hydrochloride

EIA Enzyme immunoassay

eq. equivalent

Et Ethyl

EtOAc Ethyl acetate

FC Flash Chromatography

HOBt Hydroxybenzotriazol

KHMDS Potassium hexamethyldisilazide

LAH Lithium aluminium hydride

MeOH Methanol

MPLC Medium Pressure Liquid Chromatography

NMO N-Methylmorpholine N-oxide

org. organic

PG protecting group

Ph Phenyl

RAS Renin Angiotensin System

RP18 Reversed phase column, filled with C₁₈ hydrocarbon

rt room temperature

SEM Trimethylsilylethoxymethyl

sol. Solution

TBAF Tetra-n-butylanmonium fluoride

TBDMS tert-Butyldimethylsilyl

TBDPS tert-Butyldiphenylsilyl

tBuOH tert-Butanol

tBuOK Potassium tert-butylate

Tf Trifluoromethylsulfonyl

TFA Trifluoroacetic acid

THF Tetrahydrofuran

TLC Thin Layer Chromatography

TMAD N,N,N′,N′-Tetramethylazodicarboxamide

Preparation of the Precursors(rac.)-(1R*,5S*)-9-Methyl-7-oxo-3,9-diazabicyclo[3.3.1]nonane-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (A)

(4-Benzyl-6-ethoxycarbonylmethyl-1-methyl-piperazin-2-yl)acetic acidethyl ester (Patent WO 92/05174) (71.0 g, 0.196 mol) was dissolved inMeOH (400 mL). TFA (77.8 mL, 1.02 mol) was added and the flask waspurged with nitrogen. Pd/C (10%, 50% moisture, 3.6 g) was added. Theflask was closed and purged with hydrogen (3×). After 1 day, the mixturewas filtered through Celite and washed with MeOH. The solvents wereremoved under reduced pressure and the foamy residue (92.7 g) was driedunder high vacuum. A sol. of tBuOK (117.2 g, 1.04 mol) in toluene (3.07L) was heated to reflux. A sol. of the crude piperazine formerlyobtained, dissolved in THF (300 mL), was added dropwise over 50 min. Theblack mixture was stirred for 10 further min. and allowed to cool to rt.The mixture was cooled to 0° C. and AcOH (36.6 mL, 0.635 mol) was added.The solvents were removed under reduced pressure. This crude materialwas suspended in CH₂Cl₂ (400 mL) and cooled to 0° C. DIPEA (19.1 mL, 112mmol) was added. A sol. of Boc₂O (24.3 g, 113 mmol) in CH₂Cl₂ (200 mL)was added dropwise. The mixture was stirred for 1 h at 0° C., then 1 hat rt. The mixture was washed with aq. 10% Na₂CO₃ (2×). The org.extracts were dried over MgSO₄, filtered and the solvents wereevaporated under reduced pressure. The residue was purified by FC(EtOAc/heptane 1:1→EtOAc). The title compound was obtained as oil (24.5g, 38%). R_(f)=0.05 (EtOAc/heptane 1:1) or 0.56 (MeOH/CH₂Cl₂ 1:9).LC-MS: R_(t)=2.94; ES+: 325.19.

(rac.)-(1R*,5S*)-9-Methyl-7-trifluoromethanesulfonyloxy-3,9-diazabicyclo-[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (B)

A sol. of bicyclononanone A (2.22 g, 6.80 mmol) in THF (50 mL) wascooled to 0° C. and NaH (about 60% in mineral oil, 326 mg, about 8.2mmol) was added. A gas evolution was observed. After 20 min, Tf₂NPh(3.22 g, 9.00 mmol) was added. 10 min later, the ice bath was removed.After 3 h, the sol. was diluted with EtOAc and washed with brine (1×).The org. extracts were dried over MgSO₄, filtered, and the solvents wereremoved under reduced pressure. Purification by FC (EtOAc/heptane3:1→EtOAc) yielded the title compound as an oil (2.50 g, 80%).R_(f)=0.15 (EtOAc/heptane 1:1). LC-MS: R_(t)=4.73; ES+: 458.95.

Compounds of Type C 3-(4-Bromophenyl)prop-1-yl 2-chlorophenyl ether (C1)

To a sol. of 3-(4-bromophenyl)propan-1-ol (Glover S. A., et al.;Tetrahedron, 1990, 46, 7247; 24.5 g, 0.114 mol) in toluene (600 mL)under nitrogen were added 2-chlorophenol (17.4 mL, 0.171 mmol),diisopropyl azodicarboxylate (33.1 mL, 0.171 mol) andtri-n-butylphosphine (42.2 mL, 0.171 mol). The sol. was heated to refluxand stirred under reflux overnight. The sol. was allowed to cool to rtand the solvents were removed under reduced pressure. The residue wasdiluted in EtOAc and washed with aq. 1M HCl (1×) and aq. 1M NaOH (2×).The org. extracts were dried over MgSO₄, filtered and the solvents wereremoved under reduced pressure. Purification of the residue by FC(petroleum ether→Et₂O/petroleum ether 1:99→1:19) led to the titlecompound (15.1 g, 41%). R_(f)=0.70 (EtOAc/heptane 1:3).

2-(4-Bromophenyl)eth-1-yl 2,3,5-trimethylphenyl ether (C2)

A mixture of 2-(4-bromophenyl)ethanol (20.0 mL, 143 mmol),2,3,5-trimethylphenol (31.1 g, 229 mmol), azodicarboxylic dipiperidide(72.1 g, 286 mmol) and tributylphosphine (88 mL; 357 mmol) in toluene(2.00 L) was heated to reflux for 2 h. The mixture was allowed to coolto rt. The mixture was filtered, washed with toluene and the solventswere partially removed under reduced pressure. The residue was dilutedwith Et₂O and washed with aq. 1M NaOH (2×). The org. extracts were driedover MgSO₄, filtered, and the solvents were removed under reducedpressure. Purification of the residue by FC (petroleumether→Et₂O/petroleum ether 1:3) yielded the title compound (33.1 g,73%). LC-MS: R_(t)=6.95.

1-Bromo-4-[3-(2-methoxybenzyl)propoxy]benzene (E)

4-Bromophenol (4.32 g, 25.0 mmol) and1-(3-chloropropoxymethyl)-2-methoxy-benzene (Vieira E., et al., Bioorg.Med. Chem. Letters, 1999, 9, 1397,4.88 g, 22.7 mmol.) were dissolved inDMF (150 mL). NaI (1.50 g, 0.10 mmol) and Cs₂CO₃ (16.3 g, 50.0 mmol)were added. The mixture was heated to 80° C. and stirred for 6 h, beforeit was allowed to cool to rt. After dilution with EtOAc (600 mL) themixture was washed with water (1×), aq. 1M NaOH (1×). aq. 1M HCl (1×).The org. extracts were dried over MgSO₄ and filtered. The solvents wereremoved under reduced pressure. Purification of the residue by FC(Et₂O/petroleum ether 1:9→1:4) yielded the title compound (5.66 g, 71%).R_(f)=0.60 (Et₂O/heptane 1:1).

5-Bromo-2-[3-(2-methoxybenzyloxy)propoxy]pyridine (F)

3-(5-Bromopyridin-2-yloxy)propan-1-ol (Patent Application WO 98/39328,1.05 g, 4.51 mmol) was diluted at rt in DMF (24 ml) and the sol. cooledto 0° C. NaH (55-65 weight % in mineral oil, 193 mg, 4.42-5.23 mmol) wasadded and the yellow mixture was stirred for 20 min. 2-Methoxybenzylchloride (1.49 ml, 10.7 mmol) was added and the solution was allowed towarm to rt and was stirred for 4 h. The mixture was quenched with iceand diluted with EtOAc (20 ml), washed with brine and water, dried overMgSO₄ and filtered. The solvents were evaporated under reduced pressure.Purification of the residue by FC (Et₂O, heptane 1:39→1:19) yielded thetitle compound (627 mg, 40%) as an oil. R_(f)=0.07 (Et₂O/heptane, 1:3).

Compounds of Type G(rac.)-(1R*,5S*)-9-Methyl-7-[4-(2-trimethylsilanylethoxymethoxy)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G1)

A sol. of [2-(4-bromophenoxymethoxy)ethyl]trimethylsilane (Blass B. E.,et al., Tetrahedron Lett., 2001, 42, 1611, 4.13 g, 13.6 mmol) in THF (30mL) was cooled to −78° C. BuLi (1.6 M in hexane, 9.1 mL, 14.6 mmol) wasadded. The sol. was stirred at −78° C. for 30 min. A sol. of ZnCl₂,prepared from ZnCl₂ (2.23 g, about 16.4 mmol) dried under high vacuumfor 2 h at 140° C. and THF (35 mL), was added and the resulting sol. wasallowed to warm up to rt. A sol. of bicyclononene B (2.50 g, 5.45 mmol)in THF (5 mL) and then Pd(PPh₃)₄ (157 mg, 0.136 mmol) were added. After10 min, the reaction mixture was heated to reflux. After 90 min, thereaction mixture was allowed to cool to rt and quenched with aq. 1M HCl.The mixture was diluted with EtOAc and washed with aq. 10% Na₂CO₃ (1×).The org. extracts were dried over MgSO₄ and filtered. The solvents wereremoved under reduced pressure. Purification of the residue by FC(MeOH/CH₂Cl₂ 1:39→1:24→1:20) yielded the title compound as an oil (2.90g, 99%). R_(f)=0.39 (MeOH/CH₂Cl₂ 1:9). LC-MS: R_(t)=4.35; ES+: 533.29.

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldimethylsilanyloxy)ethyl]phenyl}-9-me-thyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G2)

A sol. of [2-(4-bromophenyl)ethoxy]-tert-butyldimethylsilane (Fuji K.,et al., Tetrahedron Lett., 1990, 31, 6553, 21.8 g, 69.1 mmol) in THF(250 mL) was cooled to −78° C. BuLi (1.55M in hexane, 44.6 mL, 69.1mmol) was added. The sol. turned temporarily orange, then yellowish.After 30 min, ZnCl₂ (1M in THF, 70 mL, 70 mmol, prepared as describedfor G1) was added. The sol. was allowed to warm up to rt. Vinyl triflateB (12.91 g, 28.2 mmol) dissolved in THF (20 mL), and Pd(PPh₃)₄ (600 mg,0.519 mmol) were added. The sol. was stirred at rt for 90 min and aq. 1MHCl (1 mL) was then added. The mixture was diluted in EtOAc and washedwith aq. 1M NaOH (1×). The org. extracts were dried over MgSO₄,filtered, and the solvents were removed under reduced pressure.Purification of the residue by FC (MeOH/CH₂Cl₂ 1:49→1:24→3:47→2:25)yielded the title compound (10.91 g, 71%). R_(f)=0.65 (MeOH/CH₂Cl₂ 1:9).LC-MS: R_(t)=5.32, ES+: 545.49.

(rac.)-(1R*,5S*)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-9-me-thyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G3)

A sol. of [3-(4-bromophenyl)propoxy]-tert-butyldimethylsilane(Kiesewetter D. O., Tetrahedron Asymmetry, 1993, 4, 2183, 22.60 g, 68.6mmol) in THF (250 mL) was cooled to −78° C. BuLi (1.55M in hexane, 44.3mL, 68.6 mmol) was added. The sol. turned orange, then dark green. After30 min, ZnCl₂ (1M in THF, 69 mL, 69 mmol, prepared as described for G2)was added, whereas the sol. turned deep yellow. The mixture was allowedto warm up to rt. Vinyl triflate B (12.91 g, 28.2 mmol) in THF (20 mL)and then Pd(PPh₃)₄ (600 mg, 0.519 mmol) were added. The mixture wasstirred at rt for 90 min and aq. 1M HCl (1 mL) was added. The mixturewas diluted with EtOAc and washed with aq. 1M NaOH (1×). The org.extracts were dried over MgSO₄, filtered and the solvents were removedunder reduced pressure. Purification of the residue by FC (MeOH/CH₂Cl₂1:49→1:24→3:47→2:23) yielded the title product (10.76 g, 70%).R_(f)=0.60 (MeOH/CH₂Cl₂ 1:9). LC-MS: R_(t)=4.95; ES+: 559.51.

(rac.)-(1R*,5S*)-7-{6-[3-(2-Methoxybenzyloxy)propoxy]pyridin-3-yl}-9-me-thyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G4)

A sol. of bromopyridinyl derivative F (300 mg, 852 μmol) in THF (10 ml)was cooled to −78° C. BuLi (1.55M in hexane, 0.580 ml, 889 μmol) wasadded and the mixture was stirred for 30 min. ZnCl₂ (1M in THF, 0.94 ml,0.94 mmol, prepared as described for G2) was added and the reactionmixture was allowed to warm up to rt. Vinyl triflate B (259 mg, 596μmol) in THF (1 ml), was added, followed by Pd(PPh₃)₄ (20.4 mg, 16.6μmol). The mixture was refluxed for 2 h. The reaction was terminatedupon addition of ice. After dilution with EtOAc (125 ml), the reactionmixture was washed with 10% aq. Na₂CO₃ and the org. extracts were driedover MgSO₄ and filtered. The solvents were evaporated under reducedpressure. Purification of the residue by FC(CH₂Cl₂/MeOH:39:1→29:1→24:1→19:1→9:1) led to title compound (197 mg, 54%). R_(f)=0.35(CH₂Cl₂/MeOH 9:1). LC-MS: R_(t)=4.06; ES+: 582.78.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Methoxybenzyloxy)propoxy]phenyl}-9-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G5)

A sol. of bromophenyl derivative E (5.60 g, 15.9 mmol) in THF (50 mL)was cooled to −78° C. BuLi (1.55M in hexane, 10.3 mL, 15.9 mmol) wasadded. The sol. was stirred at −78° C. for 30 min and ZnCl₂ (1M in THF,17.5 mL, 17.5 mmol, prepared as described for G2) was added. Afterwarming up to rt, a sol. of vinyl triflate B (3.63 g, 7.90 mmol) in THF(5 mL), followed by Pd(PPh₃)₄ (205 mg, 0.177 mmol), were added. Themixture was heated to reflux while turning black. After 1 h, thereaction mixture was allowed to cool to rt. Ice was added and themixture was diluted in EtOAc. The org. extracts were washed with aq. 1MNaOH (1×) and dried over MgSO₄. The solvents were removed under reducedpressure. Purification of the residue by FC (MeOH/CH₂Cl₂1:49→3:97→1:24→1:19→1:9) yielded the title compound (4.57 g, 99%).R_(f)=0.50 (MeOH/CH₂Cl₂ 1:9). LC-MS: R_(t)=4.17; ES+: 581.60.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Chlorophenoxy)propyl]phenyl}-9-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G6)

A sol. of bromophenyl derivative C1 (16.0 g, 49.0 mmol) in THF (700 mL)was cooled to −78° C. BuLi (1.55M in hexane, 34.8 mL, 54.0 mmol) wasadded. The sol. was stirred at −78° C. for 30 min and ZnCl₂ (1M in THF,54.0 mL, 54.0 mmol, prepared as described for G2) was added. Afterwarming up to rt, a sol. of vinyl triflate B (15.0 g, 32.7 mmol) in THF(50 mL), followed by Pd(PPh₃)₄ (945 mg, 0.818 mmol), were added. Thesol. was heated to reflux. After 30 min, the reaction mixture wasallowed to cool to rt. Ice was added and the mixture was diluted inEtOAc. The org. phase was washed with aq. 1M NaOH (1×) and dried overMgSO₄. The solvents were removed under reduced pressure. Purification ofthe residue by FC (MeOH/CH₂Cl₂ 1:49→3:97→1:24→1:19→1:9) yielded thetitle compound (10.5 g, 58%). LC-MS: R_(t)=4.41; ES+: 555.13.

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldimethylsilanyloxy)ethoxy]phenyl}-9-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G7)

BuLi (1.6 M in hexane, 218 mL, 350 mmol) was added to a sol. of[2-(4-bromo-phenoxy)ethoxy]-tert-butyldimethylsilane (Morita, C.; etal.al.; Heterocycles, 2000, 52, 1163; 129 g, 342 mmol) in THF (1.0 L) at−78° C. The mixture was stirred for 1 h at −78° C., and ZnCl₂ (1M inTHF, 400 mL, 400 mmol, prepared as described for G2) was added. Themixture was allowed to warn up to rt. Bicyclononene B (78.4 g, 171 mmol)and Pd(PPh₃)₄ (4.94 g, 4.28 mmol) were added. The mixture was heated toreflux for 0.5 h, and was allowed to cool to rt. Aq. 1M HCl (2 mL) wasadded. The mixture was diluted with EtOAc (2 L) and washed with aq. 1MNaOH (750 mL). The aq. extracts were extracted back with EtOAc (1×). Thecombined org. extracts were dried over MgSO₄, filtered, and the solventswere removed under reduced pressure. Purification of the residue by FC(MeOH/CH₂Cl₂ 1:49→1:24→3:47→2:23) yielded the title compound (87.7 g,91%). R_(f)=0.60 (MeOH/CH₂Cl₂ 1:9). LC-MS: R_(t)=4.74; ES+: 561.41.

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldiphenylsilanyloxy)ethyl]phenyl}-9-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 3-tert-butyl ester 6-ethyl ester (G8)

BuLi (1.5 M in hexane, 13.4 mL, 20 mmol) was added to a sol.[2-(4-bromo-phenyl)ethoxy]-tert-butyldiphenylsilane (8.79 g, 20.0 mmol,prepared from 2-(4-bromophenyl)ethanol, TBDPS-Cl and imidazol in DMF) inTHF (40 mL) at −78° C. The mixture was stirred for 30 min at −78° C.,and ZnCl₂ (1M in THF, 24 mL, 24 mmol, prepared as described for G2) wasadded. The mixture was allowed to warm up to rt. Bicyclononene B (3.67g, 8.00 mmol) and Pd(PPh₃)₄ (231 mg, 0.20 mmol) were added. The mixturewas heated to 40° C. for 40 min, and was allowed to cool to rt. Aq. 1MHCl (2 mL) was added. The mixture was diluted with EtOAc and washed withaq. 1M NaOH. The aq. extracts were extracted back with EtOAc (1×). Thecombined org. extracts were dried over MgSO₄, filtered, and the solventswere removed under reduced pressure. Purification of the residue by FC(MeOH/CH₂Cl₂ 1:49→1:24→3:47→2:23) yielded the title compound (4.32 g,81%). LC-MS: R_(t)=1.06; ES+: 669.49.

Compounds of Type H(rac.)-(1R*,5S*)-7-[4-(2-Trimethylsilanylethoxymethoxy)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H1)

β,β,β-Trichloro-tert-butyl chloroformate (6.60 g, 27.5 mmol) was addedto a sol. of bicyclononene G1 (2.93 g, 5.50 mmol) in 1,2-dichloroethane(60 mL). The sol. was heated to reflux. After 3 h, the reaction mixturewas allowed to cool to rt, and the solvents were removed under reducedpressure. Purification of the residue by FC (EtOAc/heptane1:4→1:3→2:3→1:1) yielded the title compound as an oil (3.31 g, 83%).R_(f)=0.52 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.40; ES+: 742.52.

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldimethylsilanyloxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H2)

As for the preparation of compound H1, from bicyclononene G2 (10.91 g,20.0 mmol), β,β,β-trichloro-tert-butyl chloroformate (24.0 g, 100 mmol),and 1,2-dichloroethane (210 mL). Purification of the residue FC(EtOAc/heptane 1:9→1:4→2:3) yielded the title compound (13.75 g, 94%).R_(f)=0.64 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.66; ES+: 755.37.

(rac.)-(1R*,5S*)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H3)

As for the preparation of compound H1, from bicyclononene G3 (10.96 g,19.6 mmol), β,β,β-trichloro-tert-butyl chloroformate (23.5 g, 98.1mmol), and 1,2-dichloroethane (210 mL). Purification of the residue byFC (EtOAc/heptane 1:9→1:4→2:3) yielded the title compound (13.50 g,92%). R_(f)=0.58 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.79; ES+: 769.49.

(rac.)-(1R*,5S*)-7-{6-[3-(2-Methoxybenzyloxy)propoxy]pyridin3-yl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H4)

As for the preparation of compound H1, from bicyclononene G4 (373 mg,0.642 mmol), β,β,β-trichloro-tert-butyl chloroformate (770 mg, 3.11mmol), and 1,2-dichloroethane (8 mL). Purification of the residue by FC(EtOAc/heptane 1:9→1:4→1:3) yielded the title compound (382 mg, 77%).R_(f)=0.47 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.14; ES+: 770.50.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H5)

As for the preparation of compound H1, from bicyclononene G5 (4.57 g,7.87 mmol), β,β,β-trichloro-tert-butyl chloroformate (9.44 g, 39.4mmol), and 1,2-dichloroethane (100 mL). Purification of the residue byFC (EtOAc/heptane 1:9→1:4→1:1) yielded the title compound (5.35 g, 88%).R_(f)=0.46 (EtOAc/heptane 1:1).

(rac.)-(1R*,5S*)-7-{4-[3-(2-Chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H6)

As for the preparation of compound H1, from bicyclononene G6 (10.51 g,18.9 mmol), β,β,β-trichloro-tert-butyl chloroformate (22.7 g, 94.7mmol), and 1,2-dichloroethane (350 mL). Purification of the residue byFC (EtOAc/heptane 1:8→1:4→1:1) yielded the title compound (12.5 g, 88%).

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldimethylsilanyloxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H7)

As for the preparation of compound H1, from bicyclononene G7 (87.7 g,156 mmol), β,β,β-trichloro-tert-butyl chloroformate (188 g, 784 mmol),and 1,2-dichloroethane (1.75 L). Purification of the residue by FC(EtOAc/heptane 1:19→1:3) yielded the title compound (111 g, 95%).R_(f)=0.75 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.84.

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldiphenylsilanyloxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (H8)

As for the preparation of compound Hi, from bicyclononene G8 (4.32 g,6.46 mmol), β,β,β-trichloro-tert-butyl chloroformate (7.75 g, 32.3mmol), and 1,2-dichloroethane (100 mL). Purification of the residue byFC (EtOAc/heptane 1:19→1:3) yielded the title compound (4.97 g, 90%).R_(f)=0.75 (EtOAc/heptane 1:1). LC-MS: R_(t)=1.35.

Compounds of Type J(rac.)-(1R*,5S*)-6-Hydroxymethyl-7-[4-(2-trimethylsilanylethoxymethoxy)-phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (J1)

A sol. of bicyclononene H1 (3.31 g, 4.58 mmol) in CH₂Cl₂ (60 mL) wascooled to −78° C. DIBAL (1M in toluene, 10.1 mL, 10.1 mmol) was added.The sol. was stirred for 30 min at −78° C. and was then allowed to warmslowly. DIBAL (5 mL) was added again after 1.5 h (−65° C.). Later, DIBALwas added successively in 5 mL-portions until TLC displayed no morestarting material. Ice and water were then added at −50° C. The coldbath was removed and the mixture warmed slowly to rt. More CH₂Cl₂ wasadded and the mixture was washed with aq. 1M HCl. The aq. phase wasextracted with CH₂Cl₂ (1×) and the combined org. extracts were driedover MgSO₄. After filtration and evaporation of the solvents underreduced pressure, the residue was purified by FC (EtOAc/heptane1:4→1:3→2:3) to yield the title compound as an oil (1.89 g, 60%).R_(f)=0.50 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.08; ES+: 661.38, 702.83.

(rac.)-(1R*,5S*)-7-{4-2-(tert-Butyldimethylsilanyloxy)ethyl]phenyl}-6-hydro-xymethyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (J2)

To a sol. of bicyclononene H2 (1.57 g, 2.32 mmol) in CH₂Cl₂ (40 mL) at−78° C. DIBAL (1M in toluene, 5.80 mL, 5.80 mmol) was added. The sol.was stirred at −78° C. for 1 h. Ice was added, and the mixture wasallowed to warm up to rt. More CH₂Cl₂ was added and the org. extractswere washed with aq. 1M HCl (1×), dried over MgSO₄ and filtered. Thesolvents were removed under reduced pressure. Purification of theresidue by FC (EtOAc/heptane 1:3) yielded the title compound (868 mg,59%). LC-MS: R_(t)=7.38; ES+: 715.48.

(rac.)-(1R*,5S*)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-6-hy-droxymethyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (J3)

A sol. of bicyclononene H3 (2.39 g, 3.20 mmol) in CH₂Cl₂ (55 mL) wascooled to −78° C. DIBAL (1M in toluene, 8.00 mL, 8.00 mmol) was addedand the mixture was stirred at −78° C. for 1 h. Ice was added, and themixture was allowed to warm up to rt. More CH₂Cl₂ was added and the org.extracts were washed with aq. 1M HCl (1×), dried over MgSO₄ andfiltered. The solvents were removed under reduced pressure. Purificationof the residue by FC (EtOAc/heptane 1:3) yielded the title compound(1.34 g, 59%). LC-MS: R_(t)=7.59; ES+: 727.54.

(rac.)-(1R*,5S*)-6-Hydroxymethyl-7-{6-[3-(2-methoxybenzyloxy)propoxy]-pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (J4)

A sol. of bicyclononene H4 (345 mg, 0.447 mmol) in CH₂Cl₂ (10 mL) wascooled to −78° C. DIBAL (1M in toluene, 1.92 mL, 1.92 mmol) was added.The mixture was stirred at −78° C. for 1 h and again two portions ofDIBAL (0.50 mL, 0.50 mmol) were added successively. After 2 h, ice wasadded. The mixture was allowed to warm up to rt and was diluted withmore CH₂Cl₂. The org. extracts were washed with aq. 10% Na₂CO₃ (2×),dried over MgSO₄ and filtered. The solvents were removed under reducedpressure. Purification of the residue by FC (EtOAc/heptane1:4→1:3→2:3→3:1) yielded the title compound (122 mg, 37%). R_(f)=0.36(EtOAc/heptane 1:1). LC-MS: R_(t)=6.51; ES+: 728.49.

(rac.)-(1R*,5S*)-6-Hydroxymethyl-7-(4-hydroxyphenyl)-3,9-diazabicyclo-[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (K)

To a sol. of bicyclononene J1 (1.89 g, 2.79 mmol) in THF/MeOH (1:1, 20mL), a sol. of conc. H₂SO₄ (0.100 mL) in MeOH (10 mL) was added. Themixture was stirred for 3 h at rt. The reaction mixture was diluted withEtOAc, washed with brine (1×) and aq. sat. NaHCO₃ (1×). The org.extracts were dried over MgSO₄ and filtered. The solvents were removedunder reduced pressure. Crystallization of the residue fromEtOAc/heptane led to the title compound (1.03 g, 67%). R_(f)=0.14(EtOAc/heptane 1:1). LC-MS: R_(t)=5.17; ES−: 547.06.

(rac.)-(1R*,5S*)-6-Hydroxymethyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (L)

To a sol. of bicyclononene K (1.03 g, 1.87 mmol) in DMF (20 mL) wereadded NaI (280 mg, 1.87 mmol), Cs₂CO₃ (609 mg, 1.87 mmol) and then1-(3-chloropropoxymethyl)-2-methoxybenzene (Vieira E., et al., Bioorg.Med. Chem. Letters, 1999, 9, 1397, 400 mg, 1.87 mmol). The mixture wasstirred at 100° C. After 1.5 h, another portion of Cs₂CO₃ (609 mg, 1.87mmol) and 1-(3-chloropropoxymethyl)-2-methoxybenzene chloride (400 mg,1.87 mmol) were added to complete the reaction. After 1.5 h later, themixture was allowed to cool to rt and diluted with EtOAc. The org.extracts were washed with brine (1×). The org. extracts were dried overMgSO₄ and filtered. The solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane 1:4→1:3→2:3) yieldedthe title compound (1.00 g, 73%). R_(f)=0.35 (EtOAc/heptane 1:1). LC-MS:R_(t)=6.54.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Methoxybenzyloxy)propoxy]phenyl}-6-[2-(2-me-thoxyphenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (M)

To a sol. of bicyclononene L (500 mg, 0.687 mmol) in CH₂Cl₂ (10 mL) wereadded (2-methoxyphenyl)acetic acid (206 mg, 1.37 mmol), DMAP (cat.amount), DIPEA (0.230 mL, 1.34 mmol) and EDC-HCl (134 mg, 0.700 mmol).The sol. was stirred at rt for 90 min, when a second portion of DIPEA(0.100 mL, 0.584 mmol) was added. After 3 h, the reaction mixture wasdiluted in more CH₂Cl₂ and washed with water (1×). The org. extractswere dried over MgSO₄, filtered, and the solvents were removed underreduced pressure. Purification of the residue by FC (EtOAc/heptane1:4→1:3→2:3) yielded the title compound (495 mg, 82%). R_(f)=0.42(EtOAc/heptane 1:1). LC-MS: R_(t)=7.33; ES+: 897.33.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Methoxybenzyloxy)propoxy]phenyl}-6-[2-(2-me-thoxyphenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (N)

A mixture of CH₂Cl₂ (3 mL) and HCl/dioxane (4M, 1 mL) was slowly addedto bicyclononene M (495 mg, 0.585 mmol) in an ice bath. The resultingsol. was stirred at 0° C. After 1 h, HCl/dioxane (4M, 0.5 mL) was added,and 1 h later the ice bath was removed. After 75 min, the solvents wereremoved under reduced pressure and the residue dried under high vacuum.The resulting foam was estimated to contain about 80% of the titlecompound according to LC-MS and was used without further purification.LC-MS: R_(t)=4.97; ES+: 774.97.

(rac.)-(1R*,5S*)-6-[2-(2-Methoxyphenyl)acetoxymethyl]-7-{6-[3-(2-methoxy-benzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (O)

To a sol. of bicyclononene J4 (122 mg, 0.167 mmol) in CH₂Cl₂ (5 mL) wereadded (2-methoxyphenyl)acetic acid (50 mg, 0.328 mmol), DIPEA (0.126 mL,0.740 mmol), DMAP (cat. amount) and EDC-HCl (34 mg, 0.173 mmol). Themixture was stirred at rt for 3 h, then diluted in CH₂Cl₂, and washedwith washed with water (1×). The org. extracts were dried over MgSO₄ andfiltered. The solvents were removed under reduced pressure. Purificationof the residue by FC (EtOAc/heptane 1:4→1:3→2:3→1:1) yielded the titlecompound (108 mg, 74%). LC-MS: R_(t)=7.34; ES+: 876.54.

(rac.)-(1R*,5S*)-7-{6-[3-(2-Methoxybenzyloxy)propoxy]pyridin-3-yl}-6-[2-(2-methoxyphenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester dihydrochloride salt (P)

Bicyclononene O (114 mg, 0.130 mmol) was dissolved in CH₂Cl₂ (2 mL). Thesol. was cooled to −40° C. and 4M HCl/dioxane (2 mL) was added. The sol.was stirred for 50 min while warming up slowly to 0° C. and then stirredfor 1.5 h at 0° C. The solvents were rapidly removed under reducedpressure. The residue was dried under high vacuum to give the titlecompound (156 mg) as a foam that was used without further purification.LC-MS: R_(t)=4.86; ES+: 776.48.

Compounds of Type Q(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldimethylsilanyloxy)ethyl]phenyl}-6-[2-(2-methoxyphenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (Q1)

To a sol. of bicyclononene J2 (868 mg, 1.25 mmol) in CH₂Cl₂ (20 mL) wereadded (2-methoxyphenyl)acetic acid (343 mg, 2.06 mmol), DIPEA (0.652 mL,3.81 mmol), DMAP (cat. amount), and EDC.HCl (201 mg, 1.05 mmol). Themixture was stirred at rt for 1 h and EDC.HCl (73 mg, 0.38 mmol) andDIPEA (0.163 mmol, 0.952 mmol) were added again. After 30 min. thereaction mixture was diluted with CH₂Cl₂, washed with aq. 1M HCl (1×),and aq. sat. NaHCO₃ (1×). The org. extracts were dried over MgSO₄ andfiltered. The solvents were removed under reduced pressure. Purificationof the residue by FC (EtOAc/heptane 1:3) yielded the title compound (948mg, 90%). LC-MS: R_(t)=7.98; ES+: 861.51.

(rac.)-(1R*,5S*)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-6-[2-(2-methoxyphenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (Q2)

To a sol. of bicyclononene J3 (1.34 g, 1.90 mmol) in CH₂Cl₂ (30 mL),were added 2-methoxyphenylacetic acid (633 mg, 3.81 mmol), DIPEA (0.652mL, 3.81 mmol), DMAP (cat. amount), and EDC-HCl (402 mg, 2.09 mmol). Thesol. was stirred at rt for 1 h and EDC-HCl (73 mg, 0.38 mmol) and DIPEA(0.163 mmol, 0.952 mmol) were added again. After 30 min., the reactionmixture was diluted with CH₂Cl₂, washed with aq. 1M HCl (1×) and aq.sat. NaHCO₃ (1×). The org. extracts were dried over MgSO₄ and filtered.The solvents were removed under reduced pressure. Purification of theresidue by FC (EtOAc/heptane 1:3) yielded the title compound (1.47 g,90%). LC-MS: R_(t)-8.17; ES+: 875.53. Compounds of type R

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(2-hydroxyethyl)phenyl]-6-[2-(2-methoxy-phenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (R1)

Bicyclononene Q1 (948 mg, 1.13 mmol) was dissolved in CH₂Cl₂ (20 mL).The sol. was cooled to 0° C. and 4M HCl/dioxane (20 mL) was added. After2.25 h the solvents were rapidly removed under reduced pressure, and theresidue was immediately dried under high vacuum. The resulting foam wasthen dissolved in THF (55 mL) and cooled to −78° C. DIPEA (0.774 mL,4.51 mmol) and DMAP (cat. amount) were added, followed by the additionof acetyl chloride (0.064 mL, 0.91 mmol). After 2.5 h at −78° C., MeOH(20 mL) was added, and the reaction mixture was allowed to warm to rt.The reaction mixture was diluted in EtOAc, washed with aq. 1 M HCl (1×),and the org. extract were dried over MgSO₄ and filtered. The solventswere removed under reduced pressure. Purification of the residue by FC(EtOAc/heptane 1:2) yielded the title compound (651 mg, 55%). LC-MS:R_(t)=5.47; ES+: 689.05.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(3-hydroxypropyl)phenyl]-6-[2-(2-methoxy-phenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (R2)

To a sol. of bicyclononene Q2 (1.47 g, 1.72 mmol) in CH₂Cl₂ (25 mL), 4MHCl/dioxane (25 mL) was added at 0° C. After 2.25 h at 0° C. thesolvents were rapidly removed under reduced pressure, and the residuewas immediately dried under high vacuum. The resulting foam was thendissolved in THF (75 mL) and cooled to −78° C. DIPEA (1.18 mL, 6.88mmol) and DMAP (cat. amount) were added, followed by slow addition ofacetyl chloride (0.098 mL, 1.38 mmol). After 2.5 h at −78° C. MeOH (80mL) was added, and the reaction mixture was allowed to warm up to rt.After dilution with EtOAc, the mixture was washed with aq. 1 M HCl (1×)and the org. extracts were dried over MgSO₄ and filtered. The solventswere removed under reduced pressure. Purification of the residue by FC(EtOAc/heptane 1:2) yielded the title compound (651 mg, 55%).

Compounds of Type S(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (S1)

A sol. of bicyclononene H5 (5.35 g, 6.95 mmol) in CH₂Cl₂ (30 mL) wascooled to 0° C. 4M HCl/dioxane (30 mL) was added. The sol. was stirredat 0° C. for 3.5 h, the solvents were removed under reduced pressure andthe residue dried at high vacuum. The resulting foam was dissolved inTHF (100 mL) and cooled to −78° C. DIPEA (5.80 mL, 34.7 mmol) was added.A sol. of acetyl chloride (0.494 mL, 6.95 mmol) in THF (10 mL) was addedslowly. The reaction mixture was stirred at −78° C. for 90 min, thenallowed allowed to warm to rt and diluted in MeOH (5 mL), then in EtOAc.The org. extracts were washed with aq. 1M HCl (2×), aq. sat. NaHCO₃(1×), dried over MgSO₄, filtered and the solvents were removed underreduced pressure. Purification of the residue by FC (EtOAc/heptane1:4→1:3→1:1→EtOAc) yielded the title compound (3.67 g, 74%). R_(f)=0.50(EtOAc). LC-MS: 6.22; ES+: 711.31.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (S2)

As for compound SI, from H6 (10.8 g, 14.5 mmol), CH₂Cl₂ (110 mL), 4MHCl/dioxane (110 mL), THF (220 mL), DIPEA (12.4 mL, 72.6 mmol), DMAP (89mg, 0.73 mmol), acetyl chloride (1.24 mL, 17.4 mmol), and MeOH (5 mL).Purification of the residue by FC (EtOAc/heptane 1:3→1:1-EtOAc) yieldedthe title compound (8.59 g, 86%). R_(f)=0.43 (EtOAc). LC-MS: 6.32; ES+:684.99.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(2-hydroxyethyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (S3)

As for compound SI, from H2 (3.00 g, 4.08 mmol), CH₂Cl₂ (30 mL), 4MHCl/dioxane (30 mL), THF (60 mL), DMAP (25 mg, 0.204 mmol), DIPEA (2.74mL, 16.4 mmol), acetyl chloride (0.343 mL, 4.08 mmol), and MeOH (5 mL).Purification of the residue by FC (EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc1:9) led to the title compound (1.80 g, 79%). R_(f)=0.20 (EtOAc).

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(2-hydroxyethoxy)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (S4)

As for compound Si, from H7 (5.80 g, 7.73 mmol), CH₂Cl₂ (60 mL), 4MHCl/dioxane (60 mL), THF (50 mL), DMAP (47 mg, 0.384 mmol), DIPEA (5.29mL, 31.7 mmol), acetyl chloride (0.604 mL, 8.08 mmol), and MeOH (5 mL).Purification of the residue by FC (EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc1:9) led to the title compound (3.07 g, 69%). R_(f)=0.20 (EtOAc). LC-MS:R_(t) 4.80; ES+: 576.93.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(3-hydroxypropyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (S5)

As for compound SI, from H3 (5.04 g, 6.74 mmol), CH₂Cl₂ (80 mL), 4MHCl/dioxane (80 mL), THF (80 mL), without DMAP, DIPEA (4.62 mL, 27.0mmol), acetyl chloride (0.430 mL, 6.06 mmol), and MeOH (5 mL).Purification of the residue by FC (EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc1:9) led to the title compound (3.23 g, 83%). R_(f)=0.20 (EtOAc). LC-MS:R_(t)=1.00; ES+: 575.13.

Compounds of Type T(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (T1)

To a sol. of bicyclononene SI (3.67 g, 5.15 mmol) in EtOH (27 mL) wasadded aq. NaOH (1M, 27 mL, 27 mmol). The mixture was heated to 80° C.for 3 h and then allowed to cool to rt. After adjustment of the pH to1-2 with aq. 1M HCl and extraction with EtOAc (2×), the combined org.extracts were dried over MgSO₄, filtered, and evaporated under reducedpressure. Purification of the residue by FC (EtOAc/heptane1:1→3:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compound (1.45 g, 41%).LC-MS: R_(t)=5.50; ES+: 683.24.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (T2)

From bicyclononene S2 (8.59 g, 12.5 mmol) the title compound (4.29 g,52%) was obtained after purification by FC (MeOH/CH₂Cl₂1:99→1:49→3:97→1:24) as described for Ti. LC-MS: R_(t)=5.61; ES−:655.24.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(2-hydroxyethoxy)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester (T3)

From bicyclononene S4 (3.07 g, 5.73 mmol) in EtOH (119 mL) and aq. 1MNaOH (119 mL) the title compound (1.88 g, 60%) was obtained afterpurification by FC (MeOH/CH₂Cl₂ 1:99→1:49→3:97→1:24) as described forTi. LC-MS: R_(t)=4.32; ES+: 548.96.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(tert-butyldimethylsilanyloxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (T4)

A mixture of bicyclononene AZ1 (1.60 g, 2.93 mmol), imidazol (797 mg,11.7 mmol) and TBDMS-Cl (1.1 g, 7.30 mmol) in DMF (20 mL) was stirred atrt overnight. Aq. sat. NH₄Cl was added and the mixture was extractedwith hexane (3×). The combined org. extracts were dried over MgSO₄,filtered, and the solvents were evaporated under reduced pressure. Amixture of this crude product and K₂CO₃ (0.2 g) in THF (30 ml), MeOH (10ml), and H₂O (10 ml) was stirred at rt for 3 h. Aq. sat. NH₄Cl was addedand this mixture was extracted with Et₂O (3×). The combined org.extracts were dried over MgSO₄, filtered, and the solvents were removedunder reduced pressure. This yielded the title compound (1.85 g, 95%)that was used without further purification.

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldiphenylsilanyloxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (T5)

As for compound T4, but from bicyclononene AZ2 (crude, about 5.79 mmol),imidazol (1.2 g, 17.6 mmol) and TBDPS-Cl (4.84 g, 17.6 mmol) in DMF (50mL), then K₂CO₃ (0.5 g), THF (60 mL), MeOH (20 mL), and H₂O (20 mL). Thecrude title compound (9.6 g, quantitative yield) was used furtherwithout purification. LC-MS: R_(t)=1.26.

Compounds of Type U(rac.)-(1R*,5S*)-3-Acetyl-7-(4-hydroxyphenyl)-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (U1)

To a sol. of bicyclononene W1 (0.93 g, 1.37 mmol) in CH₂Cl₂ (10 mL) wasadded HCl/dioxane (10 mL) at 0° C. After 15 min, the ice bath wasremoved. The reaction mixture was stirred at rt for 1 h and the solventswere removed under reduced pressure. After drying at high vacuum for 30min., the resulting solid or foam was dissolved in THF (10 mL). DIPEA(0.983 mL, 5.48 mmol) and DMAP (cat. amount) were added. The sol. wascooled to −78° C. and a sol. of AcCl (0.0973 mL, 1.37 mmol) in THF (5mL) was slowly added over 2 min. After 75 min at −78° C. MeOH (10 mL)was added and the mixture was allowed to warm up. After dilution inEtOAc, the reaction mixture was washed with aq. 1M HCl (1×) and aq. sat.NaHCO₃ (1×). The org. extracts were dried over MgSO₄, filtered, andevaporated under reduced pressure. Purification of the residue by FC(EtOAc/heptane 1:3→1:1→3:1→EtOAc→MeOH/EtOAc 1:19→1:9) yielded the titlecompound (253 mg, 30%). R_(f)=0.30 (EtOAc). LC-MS: R_(t)=5.12; ES+:622.31.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(2-hydroxyethyl)phenyl]-6-(methylphenethyl-carbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (U2)

To a sol. of bicyclononene W2 (3.46 g, 4.88 mmol) in CH₂Cl₂ (35 mL) wasadded HCl (4M in dioxane, 35 mL) at 0° C. After 1 h the ice bath wasremoved, and stirring continued for 1 h at rt. The solvents were removedunder reduced pressure and the residue dried under high vacuum. Theresulting foam was dissolved in THF (50 mL). DIPEA (3.34 mL, 19:5 mmol)and DMAP (cat. amount) were added. The reaction mixture was cooled to−78° C. and AcCl (0.347 mL, 4.88 mmol) in THF (20 mL) was addeddropwise. After 2 h at −78° C., AcCl (0.100 mL, 1.41 mmol) was addedagain, followed by a third portion of AcCl (0.050 mL, 0.71 mmol) 1.5 hlater. MeOH (10 mL) was added after 30 min. and the mixture was allowedto warm up to rt. After dilution with EtOAc and washing with aq. 1M HCl(1×) and aq. sat. NaHCO₃ (1×), the org. extracts were dried over MgSO₄and filtered. The solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc1:9) yielded the title compound as a colorless foam (2.06 g, 65%).R_(f)=0.15 (EtOAc). LC-MS: R_(t)=5.14; ES+: 650.21.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(3-hydroxypropyl)phenyl]-6-(methylphen-ethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (U3)

To a sol. of bicyclononene W3 (3.18 g, 4.40 mmol) in CH₂Cl₂ (30 mL) wasadded HCl (4M in dioxane, 30 mL) at 0° C. After 1 h at 0° C. and 1 h atrt, the solvents were removed under reduced pressure and the residuedried under high vacuum. The residue was dissolved in THF (45 mL), andDIPEA (3.02 mL, 17.6 mmol) and DMAP (cat. amount) were added. The sol.was cooled to −78° C. and a sol. of AcCl (0.313 mL, 4.40 mmol) in THF(15 mL) was added dropwise over 5 min. After 1.25 h, AcCl (0.070 mL,0.984 mmol) was added again. After 30 min. MeOH (10 mL) was added andthe mixture was allowed to warm up to rt. After dilution in EtOAc andwashing with aq. 1M HCl (1×) and aq. sat. NaHCO₃ (1×), the org. extractswere dried over MgSO₄ and filtered. The solvents were removed underreduced pressure. Purification of the residue by FC (EtOAc/heptane1:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compound (2.92 g, 66%) as afoam. R_(f)=0.23 (EtOAc). LC-MS: R_(t)=5.24; ES+: 664.29.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(2-hydroxyethoxy)phenyl]-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (U4)

A mixture of bicyclononene T3 (1.88 g, 3.42 mmol), methylphenethylamine(1.49 mL, 10.3 mmol), DMAP (41 mg, 0.34 mmol), DIPEA (2.33 mL, 18.0mmol), HOBt (46 mg, 0.34 mmol) and EDC-HCl (1.64 g, 8.55 mmol) in CHCl₃(40 mL) was stirred overnight at rt. The mixture was diluted in CH₂Cl₂and washed with aq. 1M HCl (2×) and aq. sat. NaHCO₃. The organicextracts were dried over MgSO₄, filtered, and the solvents were removedunder reduced pressure. Purification of the residue by FC (EtOAc/heptane1:4→1:1×4:1→EtOAc) yielded the title compound (1.33 g, 58%). LC MS:R_(t)=5.25; ES+: 666.08.

Compounds of Type V(rac.)-(1R*,5S*)-7-(4-Hydroxyphenyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (V1)

To a sol. of bicyclononene H1 (4.18 g, 5.79 mmol) in EtOH (55 mL) aq.NaOH (1M, 55 mL, 55 mmol) was added. The mixture was stirred at 80° C.for 28 h before it was allowed to cool to rt and acidified to pH 1 withaq. 1M HCl. After extraction with EtOAc (3×) the combined org. extractswere dried over MgSO₄ and filtered. The solvents were removed underreduced pressure. Purification of the residue by FC (MeOH/CH₂Cl₂1:49→3:97→1:24→1:19→1:9→1:4) yielded the title compound (1.50 g, 40%).R_(f)=0.29. LC-MS: R_(t)=4.91; ES−: 561.12.

(rac.)-(1R*,5S*)-7-[4-(2-Hydroxyethyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(V2)

To a sol. of bicyclononene H2 (13.75 g, 18.7 mmol) in EtOH (180 mL) aq.NaOH (1M, 180 mL, 180 mmol) was added. The mixture was stirred at 80° C.for 8 h and then left at −5° C. overnight. The mixture was acidified topH 1 with aq. 1M HCl and extracted with EtOAc (3×). The org. extractswere dried over MgSO₄ and filtered. The solvents were removed underreduced pressure. Purification of the residue by FC (MeOH/CH₂Cl₂1:49→3:47→1:24→1:19×1:9→1:4) yielded the title compound, contaminatedwith(rac.)-(1R*,5S*)-7-[4-(2-hydroxyethyl)phenyl]-3,9-diazabicyclo[3.3.1]non-7-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(7.09 g, 64%). R_(f) 10=0.40 MeOH/CH₂Cl₂ 1:9). R_(t)=4.90; ES−: 589.16.

(rac.)-(1R*,5S*)-7-[4-(3-Hydroxypropyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (V3)

To a sol. of bicyclononene H3 (13.50 g, 18.0 mmol) in EtOH (180 mL) aq.NaOH (1M, 180 mL, 180 mmol) was added. The mixture was heated to 40° C.and after 1 h to 80° C. After 7 h, the mixture was left overnight at −5°C. EtOH (100 mL) and aq. NaOH (1M, 50 mL, 50 mmol) were added and thesol. was heated to 80° C. for 6 h. After cooling to rt and adjustment ofthe pH to 1 with aq. 1M HCl, the mixture was extracted with EtOAc (3×).The combined org. extracts were dried over MgSO₄ and filtered. Thesolvents were removed under reduced pressure. Purification of theresidue by FC (MeOH/CH₂Cl₂ 1:49→3:97→1:24→1:19→1:9→1:4) yielded thetitle compound (4.80 g, 55%). R_(f)=0.50 (MeOH/CH₂Cl₂ 1:9). LC-MS:R_(t)=4.99; ES−: 603.20.

Compounds of Type W(rac.)-(1R*,5S*)-7-(4-Hydroxyphenyl)-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (W1)

To a susp. of bicyclononene V1 (1.50 g, 2.66 mmol) in CHCl₃ (30 mL) wasadded methylphenethylamine (0.774 mL, 5.32 mmol). DMAP (32.5 mg, 0.266mmol), HOBt (36 mg, 0.266 mmol), and EDC.HCl (765 mg, 3.99 mmol) wereadded successively. After 3 days at rt the mixture was diluted in CH₂Cl₂and washed with aq. 1M HCl (1×) and aq. sat. NaHCO₃ (1×). The org.extracts were dried over MgSO₄ and filtered. The solvents were removedunder reduced pressure. Purification of the residue by FC (EtOAc/heptane1:9→1:4→3:7→2:3→1:1→3:2→7:3) yielded the title compound as a colorlesssolid (0.93 g, 51%). R_(f)=0.25 (EtOAc/heptane 1:1). LC-MS: R_(t)=5.86;ES−: 678.14.

(rac.)-(1R*,5S*)-7-[4-(2-Hydroxyethyl)phenyl]-6-(methylphenethylcarbamo-yl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (W2)

To a sol. of bicyclononene V2 (7.09 g, 11.97 mmol) in CHCl₃ (140 mL)were added N-methylphenethylamine (3.48 mL, 24.0 mmol), DMAP (137 mg,1.12 mmol), HOBt (151 mg, 1.12 mmol) and EDC-HCl (3.44 g, 18.0 mmol).The mixture was stirred at rt for 3 days, before it was diluted withCH₂Cl₂ and washed with aq. 1M HCl (1×) and aq. sat. NaHCO₃ (1×). Theorg. extracts were dried over MgSO₄ and filtered. The solvents wereremoved under reduced pressure. Purification of the residue purified byFC (MeOH/CH₂Cl₂ 1:49→3:122→4:121→1:24→1:9→1:4) yielded the titlecompound (3.46 g, 41%). R_(f)=0.26 (MeOH/CH₂Cl₂ 1:19). LC-MS:R_(t)=5.87; ES+: 708.40.

(rac.)-(1R*,5S*)-7-[4-(3-Eydroxypropyl)phenyl]-6-(methylphenethylcarba-moyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (W3)

To a sol. of bicyclononene V3 (7.59 g, 12.5 mmol) in CHCl₃ (150 mL) wereadded methylphenethylamine (3.63 mL, 25.0 mmol), DMAP (153 mg, 1.25mmol), HOBt (169 mg, 1.25 mmol) and EDC-HCl (3.80 g, 19.2 mmol). Themixture was stirred at rt for 3 days before it was diluted in CH₂Cl₂ andwashed with aq. 1M HCl (1×) and aq. sat. NaHCO₃ (1×). The org. extractswere dried over MgSO₄ and filtered. The solvents were removed underreduced pressure. Purification of the residue by FC (MeOH/CH₂Cl₂1:49→3:97→1:24→1:9→1:4) yielded the title compound (3.18 g, 35%).R_(f)=0.42 (MeOH/CH₂Cl₂ 1:19). LC-MS: R_(t)=5.99; ES+: 744.50.

(rac.)-(1R*,5S*)-3-Acetyl-6-hydroxymethyl-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (X)

To a sol. of bicyclononene Si (2.29 g, 3.21 mmol) in CH₂Cl₂ (100 mL) wasadded BF₃.Et₂O (0.460 mL, 3.66 mmol) at −78° C. The mixture was stirredat −78° C. for 30 min and DIBAL (1M in toluene, 6.42 mL, 6.42 mmol) wasadded. After 75 min, ice was added and the mixture was allowed to warmup to rt. CH₂Cl₂ was added and the mixture was washed with aq. 1M HCl(1×). The org. extracts were separated, dried over MgSO₄ and filtered.The solvents were removed under reduced pressure. Purification of theresidue by FC (EtOAc/heptane 1:2→1:1→EtOAc) yielded the title compound(1.01 g, 47%).

(rac.)-(1R*,5S*)-3-Acetyl-6-formyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (Y)

To a sol. of bicyclononene X (258 mg, 0.385 mmol) in CH₂Cl₂ (5 mL) wasadded to 0° C. Dess-Martin periodane (170 mg, 0.401 mmol) at 0° C. After45 min. at 0° C. a second portion periodane was added. The sol. wasstirred for 15 min before the solvents were removed under reducedpressure. Direct purification of the residue by FC (EtOAc/heptane2:3→1:1→3:2→7:3) yielded the title compound (188 mg, 73%). R_(f)=0.49(EtOAc). LC-MS: R_(t)=6.18; ES+: 667.21.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-6-methylaminomethyl-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (Z)

To a sol. of bicyclononene Y (334 mg, 0.50 mmol) in MeOH (10 mL)methylamine (40% in water, 0.215 mL, 2.5 mmol) was added. The mixturewas stirred at rt for 1 h and then cooled to 0° C. NaBH₄ (20 mg, 0.50mmol) was added. The mixture was stirred at rt for 4 h before K₂CO₃ (263mg) was added. After evaporation under reduced pressure the residue wasdistributed between EtOAc and water. The org. extracts were separated,dried over MgSO₄, and filtered. The solvents were removed under reducedpressure. Purification of the residue by RP18-MPLC yielded the titlecompound (130 mg, 38%). LC-MS: R_(t)=1.00; ES+: 682.14.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AA)

Bicyclononene H6 (1.71 g, 2.3 mmol) was dissolved in EtOH (50 mL). Aq.1M NaOH (50 mL) was added and the mixture was heated to 80° C. The sol.was stirred for 5 h at 80° C., then allowed to cool down to rt. Afteracidification to pH=1-2 with aq. 1M HCl the mixture was extracted withEtOAc (3×). The combined org. extracts were dried over MgSO₄, filteredand the solvents were removed under reduced pressure. Purification ofthe residue by FC (EtOAc/heptane 2:3→1:2→1:1) yielded the title compound(504 mg, 31%). R_(f)=0.30 (EtOAc/heptane 1:1). LC-MS: R_(t)=6.21; ES−:712.34.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Chlorophenoxy)propyl]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]methylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AB)

Bicyclononene AA (504 mg, 0.703 mmol) was dissolved in CHCl₃ (25 mL).[2-(2-chlorophenyl)ethyl]methylamine (Jaques B.; Wallace R. G.,Tetrahedron, 1977, 33, 581; 238 mg, 1.40 mmol), DIPEA (0.240 mL, 1.40mmol), DMAP (17 mg, 0.14 mmol), HOBt (19 mg, 0.10 mmol) and EDC-HCl (135mg, 1.40 mmol) were added. The sol. was stirred at rt overnight. Themixture was diluted with CH₂Cl₂ and washed with water (1×). The org.extracts were dried over MgSO₄ and the solvents were removed underreduced pressure. Purification of the residue by filtration throughsilica gel yielded the title compound as a yellowish foam (336 mg, 55%).

(rac.)-(1R*,5S*)-7-{4-[3-(2-Chlorophenoxy)propyl]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]methylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (ac)

Bicyclononene AB (336 mg, 0.378 mmol) was dissolved in CH₂Cl₂ (3 mL). 4MHCl/dioxane (13 mL) was added and the mixture was stirred at rt for 2 h.The solvents were removed under reduced pressure. Drying the residue athigh vacuum yielded the title compound as a colorless foam that was usedwithout further purification. LC-MS: R_(t)=5.26; ES+: 765.85.

9-Methyl-7-oxo-3,9-diazabicyclo[3.3.1]nonane-3-carboxylic acidtert-butyl ester (AE)

(4-Benzyl-6-ethoxycarbonylmethyl-1-methylpiperazin-2-yl)acetic acidethyl ester (Patent WO 92/05174) (71.0 g, 0.196 mol) was dissolved inMeOH (400 mL). TFA (77.8 mL, 1.02 mol) was added and the flask waspurged with nitrogen. Pd/C (10%, 50% moisture, 3.6 g) was added. Theflask was closed and purged with hydrogen (3×). After 1 day, the mixturewas filtered through celite and washed with MeOH. The solvent wasremoved under reduced pressure and the foamy residue (92.7 g) was driedunder high vacuum. A sol. of tBuOK (117.2 g, 1.04 mol) in toluene (3.07L) was heated to reflux. A sol. of the crude piperazine formerlyobtained, dissolved in THF (300 mL), was added dropwise over 50 min.

The black mixture was stirred for 10 further min. and allowed to cool tort. The mixture was cooled to 0° C. and AcOH (36.6 mL, 0.635 mol) wasadded. The solvents were removed under reduced pressure and the residuepurified by FC (MeOH/CH₂Cl₂ 1:9→1:4→1:3). The fractions with an R_(f)value close to 0.10 (MeOH/CH₂Cl₂ 1:9) were collected and the solventremoved under reduced pressure. The residue was dissolved in aq. 5M HCl(2 L) and the reaction mixture heated to reflux overnight. The mixturewas allowed to cool to rt, then cooled to 0° C. with an ice bath. The pHwas brought to 12 by adding carefully solid KOH. This mixture wasextracted with CH₂Cl₂ (3×). The combined org. extracts were dried overMgSO₄ and the solvents were removed under reduced pressure. The residuewas suspended in CH₂Cl₂ (400 mL) and cooled to 0° C. DIPEA (19.1 mL, 112mmol) was added. A sol. of Boc₂O (24.3 g, 113 mmol) in CH₂Cl₂ (200 mL)was added dropwise. The mixture was stirred for 1 h at 0° C., then 1 hat rt. The mixture was washed with aq. 10% Na₂CO₃ (2×). The org.extracts were dried over MgSO₄, filtered and the solvents wereevaporated under reduced pressure. The residue was purified by FC(EtOAc/heptane 1:1-EtOAc). The title compound was obtained as a solidthat could be recrystallized from heptane (15.6 g, 30%). R_(f)=0.45(MeOH/CH₂Cl₂ 1:9). LC-MS: R_(t)=1.55; ES+: 254.16.

(1R,5S)-9-Methyl-7-oxo-3,9-diazabicyclo[3.3.1]nonane-3,6-dicarboxylicacid 3-tert-butyl ester 6-methyl ester (AF)

To a susp. of (−)-bis[(S)-1-phenylethyl]amine hydrochloride (226 mg,0.864 mmol) in THF (3 mL) at 0° C. was added dropwise n-BuLi (1.6M inhexane, 1.136 mL, 1.808 mmol). The mixture was stirred for 1 h at 0° C.,then cooled to −78° C. A sol. of bicyclononane AE (200 mg, 0.786 mmol)in THF (2 mL) was added dropwise over 3 min. The reaction mixture wasstirred for 3 h at −78° C., then methylcyanoformat (0.081 mL, 1.02 mmol)was added. The reaction mixture was stirred for 30 min. at −78° C. and asol. of AgNO₃ (191 mg, 1.124 mmol) in H₂O/THF (1:1, 2 mL) was added.After 10 min., H₂O (1.5 mL) and AcOH (1.5 mL) were added and thereaction mixture was allowed to warm to rt. Ammoniac (25% in water) wasadded until the Ag-salt had completely dissolved. The reaction mixturewas extracted with EtOAc (1×) and CH₂Cl₂ (2×). The combined org.extracts were dried over MgSO₄ and the solvents were removed underreduced pressure. Purification of the residue by FC (MeOH/CH₂Cl₂ 1:14)yielded the title compound (167 mg, 68%). R_(f)=0.37 (MeOH/CH₂Cl₂ 1:9).LC-MS: R_(t)=0.76; ES+: 313.10. ee=82%.

(1R,5S)-9-Methyl-7-oxo-3,9-diazabicyclo[3.3.1]nonane-3,6-dicarboxylicacid 6-benzyl ester 3-tert-butyl ester (AG)

To a susp. of (−)-bis[(S)-1-phenylethyl]amine hydrochloride (226 mg,0.864 mmol) in THF (3 mL) at 0° C. was added dropwise n-BuLi (1.6M inhexane, 1.136 mL, 1.808 mmol). The mixture was stirred for 1 h at 0° C.,then cooled to −78° C. A sol. of bicyclononane AE (200 mg, 0.786 mmol)in THF (2 mL) was added dropwise over 3 min. The reaction mixture wasstirred for 3 h at −78° C., then methylcyanoformat (0.081 mL, 1.02 mmol)was added. The reaction mixture was stirred for 30 min. at −78° C. and asol. of AgNO₃ (191 mg, 1.124 mmol) in H₂O/THF (1:1, 2 mL) was added.After 10 min., H₂O (1.5 mL) and AcOH (1.5 mL) were added and thereaction mixture was allowed to warm to rt. Ammoniac (25% in water) wasadded until the Ag-salt had completely dissolved. The reaction mixturewas extracted with EtOAc (1×) and CH₂Cl₂ (2×). The combined org.extracts were dried over MgSO₄ and the solvents were removed underreduced pressure. Purification of the residue by FC (MeOH/CH₂Cl₂ 1:14)yielded the title compound (150 mg, 49%). R_(f)=0.50 (MeOH/CH₂Cl₂ 1:9).LC-MS: R_(t)=0.87; ES+: 389.09. ee=84%.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AH)

A sol. of bicyclononene S3 (900 mg, 1.60 mmol) in toluene (15 mL) waspurged with N₂ (4×). 2-Bromo-5-fluorophenol (0.267 mL, 2.4 mmol), TMAD(344 mg, 2.00 mmol) and tributylphosphine (1.18 mL, 4.80 mmol) wereadded and the reaction mixture was heated to reflux for 1 h. The mixturewas allowed to cool to rt, and the solvents were removed under reducedpressure. Purification of the residue by FC (EtOAc/heptane1:24→1:9→2:3-7:3) yielded the title compound (1.06 g, 90%). R_(f)=0.58(EtOAc). LC-MS: R_(t)=6.52; ES+: 733.00.

Compounds of Type AJ(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AJ1)

A mixture of bicyclononene AH (1.06 g, 1.44 mmol) in EtOH (30 mL) andaq. 1M NaOH (30 mL) was stirred efficiently at 80° C. for 2.5 h. Themixture was allowed to cool to rt, acidified with aq. 1M HCl, andextracted with EtOAc (3×). The combined org. phases were dried overMgSO₄, filtered, and the solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane1:1→3:1→EtOAc→MeOH/EtOAc 1:19→1:9) yielded the title compound (845 mg,83%). R_(f)=0.10 (EtOAc). LC-MS: R_(t)=5.78; ES−: 702.81.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AJ2)

A sol. of bicyclononene AR1 (296 mg, 0.39 mmol) in MeOH (10 mL) at 0° C.was purged with N₂ (3×). Pd/C (10%, cat. amount) was added and themixture was purged with H₂ (4×). The mixture was stirred under H₂ for 2h at 0° C., and was filtered through Celite. The solvents were removedunder reduced pressure and the residue was dried under high vacuum (200mg, 80%). It was used without further purification. LC-MS: R_(t)=5.83.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester (AJ3)

As for compound AJ2, but from AR2 (205 mg, 0.25 mmol), Pd/C (cat.amount) and MeOH (10 mL). The crude material (100 mg, 56%) was usedwithout further purification. LC-MS: R_(t)=5.81.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AJ4)

As for compound AJ1, but from bicyclononene BL (1.55 g, 2.07 mmol), EtOH(55 mL) and aq. 1M NaOH (55 mL). Purification of the residue by FC(EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compound(1.17 g, 78%). R_(f)=0.20 (EtOAc). R_(t)=6.02; ES+: 721.12.

Compounds of Type AK(rac.)-(1R*,5S*)-7-{4-[2-(2-Bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK1)

A sol. of bicyclononene W2 (1.68 g, 2.37 mmol) in toluene (50 mL) waspurged with N₂ (4×). 2-Bromo-5-fluorophenol (0.403 mL, 3.56 mmol),azodicarboxylic dipiperidide (897 mg, 3.56 mmol) and tributyl phosphine(1.62 mL, 7.12 mmol) were added. The mixture was heated to reflux for 2h. The mixture was then allowed to cool to rt and the solvents wereremoved under reduced pressure. Purification of the residue by FC(EtOAc/heptane 1:19→1:9→1:4→1:1→3:1) yielded the title compound (1.88 g,90%). R_(f)=0.80 (EtOAc). LC-MS: R_(t)=7.30.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-tri-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK2)

A mixture of bicyclononene AY1 (12.15 g, 16 mmol),(2-chlorobenzyl)-cyclopropylamine (9.08 g, 50 mmol), DIPEA (10.9 mL, 64mmol), DMAP (488 mg, 4 mmol), HOBt (2.43 g, 18 mmol) and EDC-HCl (4.60g, 24 mmol) in CH₂Cl₂ (250 mL) was stirred overnight. The mixture wasdiluted with CH₂Cl₂, and washed with aq. 1M HCl (3×) and with aq. sat.NaHCO₃ (1×). The org. extracts were dried over MgSO₄, filtered, and thesolvents were removed under reduced pressure. Purification of theresidue by FC (EtOAc/heptane 1:5→1:3→1:2) yielded the title compound(9.10 g, 63%). LC-MS: R_(t)=7.68.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AK)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), benzylcyclopropylamine (Loeppky, R. N.; et al., J. Org. Chem.,2000, 65, 96; 221 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol)in CH₂Cl₂ (7 mL). Purification by FC yielded the title compound (570 mg,88%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK4)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), (2-chlorobenzyl)ethylamine (Ishihara, Y; et al.; Chem. Pharm.Bull., 1991, 39, 3225; 255 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol),DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg,1.12 mmol) in CH₂Cl₂ (7 mL). Purification by FC yielded the titlecompound (543 mg, 82%). LC-MS: R_(t)=1.29.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK5)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-(2-fluorobenzyl)amine (248 mg, 1.50 mmol), DIPEA(0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol)and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification by FCyielded the title compound (526 mg, 79%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK6)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-(3-trifluoromethyl-benzyl)amine (Brabander, H. J.; etal.; J. Org. Chem., 1967, 32, 4053; 323 mg, 1.50 mmol), DIPEA (0.515 mL,3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) andEDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification by FC yieldedthe title compound (551 mg, 79%). LC-MS: R_(t)=1.25.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK7)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-(2-methylbenzyl)-amine (242 mg, 1.50 mmol), DIPEA(0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol)and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification by FCyielded the title compound (553 mg, 84%). LC-MS: R_(t)=1.29.

(rac.)-(1R*,5S*)-6-{Cycloproyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK8)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]amine (311 mg, 1.50mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL).Purification by FC yielded the title compound (566 mg, 82%). LC-MS:R_(t)=1.28.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK9)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-[2-(2-methoxy-phenoxy)ethyl]amine (311 mg, 1.50mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL).Purification by FC yielded the title compound (570 mg, 82%). LC-MS:R_(t)=1.28.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK10)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-(2-m-tolyloxy-ethyl)amine (287 mg, 1.50 mmol), DIPEA(0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol)and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification by FCyielded the title compound (506 mg, 74%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-6-Cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK11)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-[2-(3,4-dimethyl-phenoxy)ethyl]amine (462 mg, 1.50mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL).Purification by FC yielded the title compound (693 mg, 100%). LC-MS:R_(t)=1.28.

(rac.)-(1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK12)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropylphenethylamine (Smith, P. W.; et al.; J. Med. Chem.,1998, 41, 787; 242 mg, 1.50 mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol)in CH₂Cl₂ (7 mL). Purification by FC yielded the title compound (510 mg,77%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK13)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), [2-(2-chlorophenyl)ethyl]-cyclopropylamine (294 mg, 1.50 mmol),DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75mmol) and EDC.HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification byFC yielded the title compound (540 mg, 79%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK14)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]amine (296 mg, 1.50mmol), DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101mg, 0.75 mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL).Purification by FC yielded the title compound (572 mg, 83%). LC-MS:R_(t)=1.28.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK15)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-[2-(4-fluoro-phenyl)ethyl]amine (269 mg, 1.50 mmol),DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification byFC yielded the title compound (533 mg, 79%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK16)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-(2-o-tolylethyl)-amine (263 mg, 1.50 mmol), DIPEA(0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol)and EDC.HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification by FCyielded the title compound (562 mg, 84%). LC-MS: R_(t)=1.29.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK17)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-(3,5-dimethoxy-benzyl)amine (311 mg, 1.50 mmol),DIPEA (0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75mmol) and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification byFC yielded the title compound (530 mg, 76%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK18)

As for bicyclononene AK2, but from bicyclononene AY1 (552 mg, 0.75mmol), cyclopropyl-(2-p-tolylethyl)-amine (263 mg, 1.50 mmol), DIPEA(0.515 mL, 3.00 mmol), DMAP (23 mg, 0.19 mmol), HOBt (101 mg, 0.75 mmol)and EDC-HCl (216 mg, 1.12 mmol) in CH₂Cl₂ (7 mL). Purification by FCyielded the title compound (530 mg, 79%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK19)

As for bicyclononene AK2, but from bicyclononene AY1 (1.30, 1.77 mmol),(2-alkylbenzyl)cyclopropyl-amine (992 mg, 5.30 mmol), DIPEA (1.01 mL,7.08 mmol), DMAP (54 mg, 0.44 mmol), HOBt (263 mg, 1.95 mmol) andEDC-HCl (509 mg, 2.66 mmol) in CH₂Cl₂ (25 mL). Purification by FCyielded the intermediate compound (1.49 g, 93%). LC-MS: R_(t)=7.81.

Then as for compound AT, but from the former intermediate compound (1.49g, 1.65 mmol), NMO-H₂O (245 mg, 1.82 mmol), and OsO₄ (2.5% in tert-BuOH,0.207 mL, 0.017 mmol) in THF (4 mL), tert-BuOH (2 mL) and water (1 mL).Purification of the residue by FC (EtOAc/heptane 1:4→2:3→3:2→4:1→EtOAc)yielded the 2^(nd) intermediate compound (866 mg, 56%). R_(f)=0.50(EtOAc). LC-MS: R_(t)=6.95.

Then as for compound AU, but from the 2^(nd) intermediate compound (866mg, 0.922 mmol) and NaIO₄ (217 mg, 1.01 mmol) in THF (8 mL) and water (2mL). Purification of the residue by FC (EtOAc/heptane 1:4-2:3) yieldedthe 3^(rd) intermediate compound (751 mg, 90%). R_(f)=0.75 (EtOAc).

Finally as for compound AV, but from the 3^(rd) intermediate compound(751 mg, 0.828 mmol) and NaBH₄ (35 mg, 0.9 mmol) in MeOH (10 mL).Purification of the residue by FC (EtOAc/heptane 2:3) yielded the titlecompound (599 mg, 80%). LC-MS: R_(t)=7.30.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK20)

As for bicyclononene AK2, but from bicyclononene AY2 (7.68 g, 9.86mmol), (2-chlorobenzyl)cyclopropylamine (5.37, 29.6 mmol), DIPEA (6.75mL, 39.4 mmol), DMAP (301 mg, 2.47 mmol), HOBt (1.46 mg, 10.8 mmol) andEDC-HCl (2.84 g, 14.8 mmol) in CH₂Cl₂ (150 mL). Purification by FC(EtOAc/heptane 1:4→3:7→2:3→1:1) yielded the title compound (3.7 g, 40%).R_(f)=0.55 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.97.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK21)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), benzylcyclopropylamine (Loeppky, R. N.; et al., J. Org. Chem.,2000, 65, 96; 1.27 g, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDC.HCl (287 mg, 1.50 mmol)in CH₂Cl₂ (10 mL). Purification by FC yielded the title compound (520mg, 57%). LC-MS: R_(t)=7.79.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK22)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), (2-chlorobenzyl)ethylamine (Ishihara, Y; et al.; Chem. Pharm.Bull., 1991, 39, 3225; 254 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol),DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDC.HCl (287 mg,1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FC yielded the titlecompound (475 mg, 51%). LC-MS: R_(t)=7.82.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK23)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(2-fluorobenzyl)amine (247 mg, 1.50 mmol), DIPEA(0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (465 mg, 50%). LC-MS: R_(t)=7.69.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK24)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(3-trifluoromethylbenzyl)amine (Brabander, H. J.; etal.; J. Org. Chem., 1967, 32, 4053; 323 mg, 1.50 mmol), DIPEA (0.684 mL,4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) andEDC.HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (345 mg, 35%). LC-MS: R_(t)=7.76.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK5)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(2-methylbenzyl)amine (242 mg, 1.50 mmol), DIPEA(0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)and EDC.HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (722 mg, 78%). LC-MS: R_(t)=7.77.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK26)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(4-methoxyphenoxymethyl)amine (311 mg, 1.50 mmol),DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (579 mg, 60%). LC-MS: R_(t)=7.64.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) esterAK27)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-m-tolyloxymethylamine (311 mg, 1.50 mmol), DIPEA(0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (340 mg, 36%). LC-MS: R_(t)=7.83.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK28)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(3,4-dimethylphenoxymethyl)amine (308 mg, 1.50 mmol),DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (470 mg, 49%). LC-MS: R_(t)=7.93.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK29)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-phenethylamine (Smith, P. W.; et al.; J. Med. Chem.,1998, 41, 787; 242 mg, 1.50 mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol)in CH₂Cl₂ (10 mL). Purification by FC yielded the title compound (449mg, 49%). LC-MS: R_(t)=7.72.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK30)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00 mmol), [2-(2-chloro-phenyl)ethyl]cyclopropylamine (294 mg, 1.50 mmol),DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (287 mg, 1.50 mmol). in CH₂Cl₂ (10 mL). Purificationby FC yielded the title compound (605 mg, 63%). LC-MS: R_(t)=7.89.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK31)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amine (296 mg, 1.50mmol), DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135mg, 1.00 mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL).Purification by FC yielded the title compound (670 mg, 70%). LC-MS:R_(t)=7.70.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK32)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-[2-(4-fluorophenyl)ethyl]amine (269 mg, 1.50 mmol),DIPEA (0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (638 mg, 68%). LC-MS: R_(t)=7.70.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK33)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(2-o-tolylethyl)amine (263 mg, 1.50 mmol), DIPEA(0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (659 mg, 70%). LC-MS: R_(t)=7.58.

1:1 Mixture of(rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester and(rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methyl-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK34)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), (rac.)-2-methylamino-1-phenylethanol (310 mg, 1.50 mmol), DIPEA(0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)and EDC.HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compounds (456 mg, 50%). LC-MS: R_(t)=7.42.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK35)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(3,5-dimethoxybenzyl)amine (311 mg, 1.50 mmol), DIPEA(0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (736 mg, 76%). LC-MS: R_(t)=7.73.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK36)

As for bicyclononene AK2, but from bicyclononene AY2 (779 mg, 1.00mmol), cyclopropyl-(2-p-tolylethyl)amine (263 mg, 1.50 mmol), DIPEA(0.684 mL, 4.00 mmol), DMAP (30 mg, 0.25 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (287 mg, 1.50 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (718 mg, 77%). LC-MS: R_(t)=7.73.

(rac.)-(1R*,5S*)-6-[(2-Allylbenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK37)

As for bicyclononene AK2, but from bicyclononene AY2 (1.45, 2.00 mmol),(2-allylbenzyl)cyclopropylamine (1.12 g, 6.00 mmol), DIPEA (1.37 mL,8.00 mmol), DMAP (62 mg, 0.50 mmol), HOBt (298 mg, 2.20 mmol) andEDC.HCl (576 mg, 3.00 mmol) in CH₂Cl₂ (20 mL). Purification by FCyielded the intermediate compound (1.77 g, 93%). LC-MS: R_(t)=7.95.

Then as for compound AT, but from the former intermediate compound (1.77g, 1.86 mmol), NMO-H₂O (516 mg, 3.82 mmol), and OsO₄ (2.5% in tert-BuOH,0.276 mL, 0.023 mmol) in THF (40 mL), tert-BuOH (20 mL) and water (10mL). Purification of the residue by FC (EtOAc/heptane1:4→2:3→3:2→4:1→EtOAc) yielded the 2^(nd) intermediate compound (548 mg,27%). R_(f)=0.60 (EtOAc). LC-MS: R_(t)=7.43; ES+: 980.18.

Then as for compound AU, but from the 2^(nd) intermediate compound (928mg, 0.945 mmol) and NaIO₄ (222 mg, 1.04 mmol) in THF (8 mL) and water (2mL). Purification of the residue by FC (EtOAc/heptane 1:4→2:3) yieldedthe 3^(rd) intermediate compound (868 mg, 97%). R_(f)=0.80 (EtOAc).

Finally as for compound AV, but from the 3^(rd) intermediate compound(868 mg, 0.914 mmol) and NaBH₄ (38 mg, 1.0 mmol) in MeOH (10 mL).Purification of the residue by FC (EtOAc/heptane 2:3) yielded the titlecompound (603 mg, 69%). LC-MS: R_(t)=7.44.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK38)

As for bicyclononene AK, but from bicyclononene AY3 (411 mg, 0.58 mmol),(2-chlorobenzyl)-cyclopropylamine (211 mg, 1.16 mmol), DIPEA (0.397 mL,2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and EDC.HCl(167 mg, 0.87 mmol) in CH₂Cl₂ (8 mL). Purification by FC yielded thetitle compound (312 mg, 62%). LC-MS: R_(t)=7.66.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK39)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), benzyl-cyclopropylamine (Loeppky, R. N.; et al., J. Org. Chem.,2000, 65, 96; 171 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol), DMAP (18mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl (167 mg, 0.87 mmol)in CH₂Cl₂ (8 mL). Purification by FC yielded the title compound (340 mg,70%). LC-MS: R_(t)=8.12.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK40)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), (2-chlorobenzyl)-ethylamine (Ishihara, Y; et al.; Chem. Pharm.Bull., 1991, 39, 3225; 197 mg, 1.16 mmol), DIPEA (0.397 mL, 2.32 mmol),DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl (167 mg,0.87 mmol) in CH₂Cl₂ (8 mL). Purification by FC yielded the titlecompound (374 mg, 74%). LC-MS: R_(t)=8.30.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-(2,3,5-tri-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9dicarboxy-licacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK41)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), cyclopropyl-(2-fluorobenzyl)amine (192 mg, 1.16 mmol), DIPEA(0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol)and EDC-HCl (167 mg, 0.87 mmol) in CH₂Cl₂ (8 mL). Purification by FCyielded the title compound (350 mg, 70%). LC-MS: R_(t)=8.13.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK42)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), cyclopropyl-(3-trifluoromethylbenzyl)amine (Brabander, H. J.; etal.; J. Org. Chem., 1967, 32, 4053; 250 mg, 1.16 mmol), DIPEA (0.397 mL,2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol) and EDC-HCl(167 mg, 0.87 mmol) in CH₂Cl₂ (8 mL). Purification by FC yielded thetitle compound (294 mg, 56%). LC-MS: R_(t)=8.16.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK43)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), cyclopropyl-(2-methylbenzyl)amine (187 mg, 1.16 mmol), DIPEA(0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol)and EDC.HCl (167 mg, 0.87 mmol) in CH₂Cl₂ (8 mL). Purification by FCyielded the title compound (294 mg, 56%). LC-MS: R_(t)=8.15.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK44)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amine (187 mg, 1.16 mmol),DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64mmol) and EDC.HCl (167 mg, 0.87 mmol) in CH₂Cl₂ (8 mL). Purification byFC yielded the title compound (159 mg, 30%). LC-MS: R_(t)=7.93.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK45)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), cyclopropyl-[2-(3-methoxyphenoxy)ethyl]amine (287 mg, 1.16 mmol),DIPEA (0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64mmol) and EDC-HCl (167 mg, 0.87 mmol) in CH₂Cl₂ (8 mL). Purification byFC yielded the title compound (237 mg, 45%). LC-MS: R_(t)=7.69.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK46)

As for bicyclononene AK2, but from bicyclononene AY3 (411 mg, 0.58mmol), cyclopropyl-(2-m-tolyloxyethyl)amine (222 mg, 1.16 mmol), DIPEA(0.397 mL, 2.32 mmol), DMAP (18 mg, 0.15 mmol), HOBt (86 mg, 0.64 mmol)and EDC-HCl (167 mg, 0.87 mmol) in CH₂Cl₂ (8 mL). Purification by FCyielded the title compound (185 mg, 36%). LC-MS: R_(t)=8.12.

(rac.)-(1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,6-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK47)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), cyclopropyl-phenethylamine (Smith, P. W.; et al.; J. Med. Chem.,1998, 41, 787; 402 mg, 2.49 mmol), DIPEA (0.568 mL, 3.32 mmol), DMAP (25mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol) and EDC-HCl (239 mg, 1.25 mmol)in CH₂Cl₂ (10 mL). Purification by FC yielded the title compound (309mg, 44%). LC-MS: R_(t)=8.01.

(rac.)-(1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK48)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), [2-(2-chloro-phenyl)ethyl]cyclopropylamine (487 mg, 2.49 mmol),DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25mmol) and EDC-HCl (239 mg, 1.25 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (272 mg, 37%). LC-MS: R_(t)=8.20.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK49)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amine (491 mg, 2.49mmol), DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169mg, 1.25 mmol) and EDC-HCl (239 mg, 1.25 mmol) in CH₂Cl₂ (10 mL).Purification by FC yielded the title compound (309 mg, 42%). LC-MS:R_(t)=7.98.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK50)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), cyclopropyl-[2-(4-fluorophenyl)ethyl]amine (491 mg, 2.49 mmol),DIPEA (0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25mmol) and EDC-HCl (239 mg, 1.25 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (294 mg, 41%). LC-MS: R_(t)-7.93.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK51)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), cyclopropyl-(2-o-tolylethyl)amine (491 mg, 2.49 mmol), DIPEA(0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol)and EDC.HCl (239 mg, 1.25 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (258 mg, 36%). LC-MS: R_(t)=8.16.

1:1-Mixture of(rac.)-1R*,5S*)-6-[((2R*)-2-hydroxy-2-phenylethyl)methyl-carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester and(rac.)-(1R*,5S*)-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK52)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), (rac.)-2-methylamino-1-phenylethanol (377 mg, 2.49 mmol), DIPEA(0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol)and EDC-HCl (239 mg, 1.25 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compounds (117 mg, 17%). LC-MS: R_(t)=7.50.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK53)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), cyclopropyl-(3,5-dimethoxybenzyl)amine (516 mg, 2.49 mmol), DIPEA(0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg. 1.25 mmol)and EDC-HCl (239 mg, 1.25 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (258 mg, 35%). LC-MS: R_(t)=7.80.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK54)

As for bicyclononene AK2, but from bicyclononene AY3 (590 mg, 0.83mmol), cyclopropyl-(2-p-tolylethyl)amine (426 mg, 2.49 mmol), DIPEA(0.568 mL, 3.32 mmol), DMAP (25 mg, 0.21 mmol), HOBt (169 mg, 1.25 mmol)and EDC-HCl (239 mg, 1.25 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (235 mg, 32%). LC-MS: R_(t)=8.16.

(rac.)-(1R*,5S*)-6-Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK55)

As for bicyclononene AK2, but from bicyclononene AY3 (1.18 g, 1.66mmol), (2-allylbenzyl)cyclopropylamine (932 mg, 4.98 mmol), DIPEA (1.14mL, 6.64 mmol), DMAP (51 mg, 0.42 mmol), HOBt (338 mg, 2.50 mmol) andEDC.HCl (478 mg, 2.50 mmol) in CH₂Cl₂ (20 mL). Purification by FCyielded the intermediate compound (613 mg, 42%). LC-MS: R_(t)=8.16.

Then as for compound AT, but from the former intermediate compound (613mg, 0.697 mmol), NMO-H₂O (141 mg, 1.05 mmol), and OsO₄ (2.5% intert-BuOH, 0.175 mL, 0.014 mmol) in THF (8 mL), tert-BuOH (4 mL) andwater (2 mL). Purification of the residue by FC (EtOAc/heptane1:1-EtOAc) yielded the 2^(nd) intermediate compound (348 mg, 55%).R_(f)=0.05 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.31.

Then as for compound AU, but from the 2^(nd) intermediate compound (348mg, 0.381 mmol) and NaIO₄ (122 mg, 0.571 mmol) in THF (6 mL) and water(2 mL). Drying the residue under high vacuum yielded the 3^(rd)intermediate compound (269 mg, 80%) that was used without furtherpurification. LC-MS: R_(t)=7.29. Finally as for compound AV, but fromthe 3^(rd) intermediate compound (269 mg, 0.305 mmol) and NaBH₄ (13 mg,0.34 mmol) in MeOH (5 mL). Purification of the residue by FC(EtOAc/heptane 1:4→2:3→3:2→4:1) yielded the title compound (210 mg,78%). LC-MS: R_(t)=7.55.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK56)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), (2-chlorobenzyl)-cyclopropylamine (290 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compound (451 mg, 74%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK57)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), (2-chlorobenzyl)-ethylamine (Ishihara, Y; et al.; Chem. Pharm.Bull., 1991, 39, 3225; 290 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol),DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg,1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FC yielded the titlecompound (596 mg, 83%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK58)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-(2-fluorobenzyl)amine (264 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC.HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compound (519 mg, 73%). LC-MS: R_(t)=1.29.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK59)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-(3-trifluoromethylbenzyl)amine (Brabander, H. J.; etal.; J. Org. Chem., 1967, 32, 4053; 344 mg, 1.60 mmol), DIPEA (0.548 mL,3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl(307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FC yielded thetitle compound (584 mg, 78%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK60)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-(2-methylbenzyl)amine (258 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compound (569 mg, 48%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK61)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amine (332 mg, 1.60 mmol),DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification byFC yielded the title compound (591 mg, 79%). LC-MS: R_(t)−1.28.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK62)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-[2-(3-methoxyphenoxy)ethyl]amine (332 mg, 1.60 mmol),DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification byFC yielded the title compound (584 mg, 77%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK63)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-(2-p-tolyloxyethyl)amine (306 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compound (525 mg, 71%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK64)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-phenethylamine (Smith, P. W.; et al.; J. Med. Chem.,1998, 41, 787; 258 mg, 1.60 mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol) and EDC-HCl (307 mg, 1.55 mmol)in CH₂Cl₂ (5 mL). Purification by FC yielded the title compound (360 mg,50%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK65)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), [2-(2-chloro-phenyl)ethyl]cyclopropylamine (313 mg, 1.60 mmol),DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification byFC yielded the title compound (572 mg, 76%). LC-MS: R_(t)=1.30.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK66)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amine (316 mg, 1.60mmol), DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135mg, 1.00 mmol) and EDC.HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL).Purification by FC yielded the title compound (584 mg, 79%). LC-MS:R_(t)=1.29.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK67)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-[2-(4-fluorophenyl)ethyl]amine (287 mg, 1.60 mmol),DIPEA (0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00mmol) and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification byFC yielded the title compound (616 mg, 84%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK68)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-(2-o-tolylethyl)amine (280 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compound (556 mg, 76%). LC-MS: R_(t)=1.28.

1:1-Mixture of(rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester and(rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methyl-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK69)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), (rac.)-2-methylamino-1-phenylethanol (242 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compounds (380 mg, 54%). LC-MS: R_(t)=1.23.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK70)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-(3,5-dimethoxybenzyl)amine (332 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC-HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compound (619 mg, 83%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK71)

As for bicyclononene AK2, but from bicyclononene AY4 (596 mg, 0.80mmol), cyclopropyl-(2-p-tolylethyl)amine (280 mg, 1.60 mmol), DIPEA(0.548 mL, 3.2 mmol), DMAP (25 mg, 0.21 mmol), HOBt (135 mg, 1.00 mmol)and EDC.HCl (307 mg, 1.55 mmol) in CH₂Cl₂ (5 mL). Purification by FCyielded the title compound (619 mg, 83%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AK72)

As for bicyclononene AK2, but from bicyclononene AY3 (1.00 g, 1.34mmol), (2-allylbenzyl)cyclopropylamine (752 mg, 4.02 mmol), DIPEA (0.918mL, 5.26 mmol), DMAP (41 mg, 0.34 mmol), HOBt (199 mg, 1.47 mmol) andEDC-HCl (385 mg, 2.01 mmol) in CH₂Cl₂ (15 mL). Purification by FCyielded the intermediate compound (845 mg, 69%). R_(f)=0.45(EtOAc/heptane 1:1). LC-MS: R_(t)=7.85.

Then as for compound AT, but from the former intermediate compound (845mg, 0.926 mmol), NMO.H₂O (150 mg, 1.11 mmol), and OsO₄ (2.5% intert-BuOH, 0.173 mL, 0.014 mmol) in THF (8 mL), tert-BuOH (4 mL) andwater (2 mL). Purification of the residue by FC (EtOAc/heptane1:1→EtOAc→MeOH/EtOAc 1:9) yielded the 2^(nd) intermediate compound (616mg, 70%). R_(f)=0.05 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.04.

Then as for compound AU, but from the 2^(nd) intermediate compound (616mg, 0.649 mmol) and NaIO₄ (208 mg, 0.973 mmol) in THF (6 mL) and water(2 mL). Drying the residue under high vacuum yielded the 3^(rd)intermediate compound (477 mg, 80%) that was used without furtherpurification. LC-MS: R_(t)=7.43. Finally as for compound AV, but fromthe 3^(rd) intermediate compound (477 mg, 0.520 mmol) and NaBH₄ (22 mg,0.57 mmol) in MeOH (5 mL). Purification of the residue by FC(EtOAc/heptane 1:4→2:3→3:2→4:1) yielded the title compound (210 mg,78%). R_(f)=0.10 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.26.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[(2-chloro-benzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK73)

As for bicyclononene AK2, but from bicyclononene AY5 (534 mg, 0.7 mmol),(2-chlorobenzyl)-cyclopropylamine (200 mg, 1.10 mmol), DIPEA (0.479 mL,2.8 mmol), DMAP (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC.HCl(211 mg, 1.1 mmol) in CH₂Cl₂ (7 mL). Purification by FC yielded thetitle compound (263 mg, 39%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[2-(4-bromophenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK74)

As for bicyclononene AK2, but from bicyclononene AY5 (534 mg, 0.7 mmol),benzylcyclopropyl-amine (Loeppky, R. N.; et al., J. Org. Chem., 2000,65, 96; 162 mg, 1.10 mmol), DIPEA (0.479 mL, 2.8 mmol), DMAP (21 mg,0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC-HCl (211 mg, 1.1 mmol) inCH₂Cl₂ (7 mL). Purification by FC yielded the title compound (263 mg,39%). LC-MS: R_(t)=1.26.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[(2-chloro-benzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK75)

As for bicyclononene AK2, but from bicyclononene AY5 (534 mg, 0.7 mmol),(2-chlorobenzyl)-ethylamine (Ishihara, Y; et al.; Chem. Pharm. Bull.,1991, 39, 3225; 187 mg, 1.10 mmol), DIPEA (0.479 mL, 2.8 mmol), DMAP (21mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC-HCl (211 mg, 1.1 mmol)in CH₂Cl₂ (7 mL). Purification by FC yielded the title compound (204 mg,32%). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK76)

As for bicyclononene AK2, but from bicyclononene AY5 (534 mg, 0.7 mmol),cyclopropyl-(2-fluorobenzyl)amine (182 mg, 1.10 mmol), DIPEA (0.479 mL,2.8 mmol), DMAP (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC-HCl(211 mg, 1.1 mmol) in CH₂Cl₂ (7 mL). Purification by FC yielded thetitle compound (233 mg, 37%). LC-MS: R_(t)=1.27.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK77)

As for bicyclononene AK2, but from bicyclononene AY5 (534 mg, 0.7 mmol),cyclopropyl-(3-trifluoromethylbenzyl)amine (Brabander, H. J.; et al.; J.Org. Chem., 1967, 32, 4053; 237 mg, 1.10 mmol), DIPEA (0.479 mL, 2.8mmol), DMAP (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC-HCl(211 mg, 1.1 mmol) in CH₂Cl₂ (7 mL). Purification by FC yielded thetitle compound (276 mg, 41%). LC-MS: R_(t)=1.27.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK78)

As for bicyclononene AK2, but from bicyclononene AY5 (534 mg, 0.7 mmol),cyclopropyl-(2-methylbenzyl)amine (178 mg, 1.10 mmol), DIPEA (0.479 mL,2.8 mmol), DMAP (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol) and EDC.HCl(211 mg, 1.1 mmol) in CH₂Cl₂ (7 mL). Purification by FC yielded thetitle compound (171 mg, 27%). LC-MS: R_(t)=1.26.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK79)

As for bicyclononene AK2, but from bicyclononene AY5 (534 mg, 0.7 mmol),cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amine (228 mg, 1.10 mmol), DIPEA(0.479 mL, 2.8 mmol), DMAP (21 mg, 0.18 mmol), HOBt (113 mg, 0.84 mmol)and EDC-HCl (211 mg, 1.1 mmol) in CH₂Cl₂ (7 mL). Purification by FCyielded the title compound (190 mg, 29%). LC-MS: R_(t)=1.26.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK80)

As for bicyclononene AK2, but from bicyclononene AY5 (700 mg, 0.918mmol), cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amine (565 mg, 2.75mmol), DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136mg, 1.01 mmol) and EDC.HCl (264 mg, 1.38 mmol) in CH₂Cl₂ (10 mL).Purification by FC yielded the title compound (199 mg, 23%). LC-MS:R_(t)=7.76.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK81)

As for bicyclononene AK2, but from bicyclononene AY5 (700 mg, 0.918mmol), [2-(2-chloro-phenyl)ethyl]cyclopropylamine (538 mg, 2.75 mmol),DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01mmol) and EDC-HCl (264 mg, 1.38 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (256 mg, 30%). LC-MS: R_(t)=7.70.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK82)

As for bicyclononene AK2, but from bicyclononene AY5 (700 mg, 0.918mmol), cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amine (542 mg, 2.75mmol), DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136mg, 1.01 mmol) and EDC-HCl (264 mg, 1.38 mmol) in CH₂Cl₂ (10 mL).Purification by FC yielded the title compound (245 mg, 28%). LC-MS:R_(t)=7.55.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicar-boxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK83)

As for bicyclononene AK2, but from bicyclononene AY5 (700 mg, 0.918mmol), cyclopropyl-[2-(4-fluorophenyl)ethyl]amine (493 mg, 2.75 mmol),DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01mmol) and EDC.HCl (264 mg, 1.38 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (220 mg, 26%). LC-MS: R_(t)=7.51.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK84)

As for bicyclononene AK2, but from bicyclononene AY5 (700 mg, 0.918mmol), cyclopropyl-(2-o-tolylethyl)amine (482 mg, 2.75 mmol), DIPEA(0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol)and EDC-HCl (264 mg, 1.38 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (252 mg, 30%). LC-MS: R_(t)=7.66.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK85)

As for bicyclononene AK2, but from bicyclononene AY5 (700 mg, 0.918mmol), Cyclopropyl-(3,5-dimethoxy-benzyl)-amine (570 mg, 2.75 mmol),DIPEA (0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01mmol) and EDC-HCl (264 mg, 1.38 mmol) in CH₂Cl₂ (10 mL). Purification byFC yielded the title compound (242 mg, 28%). LC-MS: R_(t)=7.42.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK86)

As for bicyclononene AK2, but from bicyclononene AY5 (700 mg, 0.918mmol), cyclopropyl-(2-p-tolylethyl)amine (482 mg, 2.75 mmol), DIPEA(0.628 mL, 3.67 mmol), DMAP (28 mg, 0.23 mmol), HOBt (136 mg, 1.01 mmol)and EDC-HCl (264 mg, 1.38 mmol) in CH₂Cl₂ (10 mL). Purification by FCyielded the title compound (246 mg, 29%). LC-MS: R_(t)=7.66.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AK87)

As for bicyclononene AK2, but from bicyclononene AY5 (1.00 g, 1.31mmol), (2-allylbenzyl)cyclopropylamine (752 mg, 4.02 mmol), DIPEA (0.918mL, 5.26 mmol), DMAP (41 mg, 0.34 mmol), HOBt (199 mg, 1.47 mmol) andEDC-HCl (385 mg, 2.01 mmol) in CH₂Cl₂ (15 mL). Purification by FCyielded the intermediate compound (875 mg, 72%). R_(f)=0.45(EtOAc/heptane 1:1). LC-MS: R_(t)=7.69.

Then as for compound AT, but from the former intermediate compound (875mg, 0.939 mmol), NMO.H₂O (152 mg, 1.13 mmol), and OsO₄ (2.5% intert-BuOH, 0.236 mL, 0.019 mmol) in THF (8 mL), tert-BuOH (4 mL) andwater (2 mL). Purification of the residue by FC (EtOAc/heptane1:1→EtOAc→MeOH/EtOAc 1:9) yielded the 2^(nd) intermediate compound (310mg, 34%). R_(f)=0.05 (EtOAc/heptane 1:1). LC-MS: R_(t)=6.86.

Then as for compound AU, but from the 2^(nd) intermediate compound (310mg, 0.321 mmol) and NaIO₄ (139 mg, 0.481 mmol) in THF (6 mL) and water(2 mL). Drying the residue under high vacuum yielded the 3^(rd)intermediate compound (239 mg, 80%) that was used without furtherpurification. LC-MS: R_(t)=7.29. Finally as for compound AV, but fromthe 3^(rd) intermediate compound (239 mg, 0.256 mmol) and NaBH₄ (11 mg,0.28 mmol) in MeOH (5 mL). Purification of the residue by FC(EtOAc/heptane 1:4→2:3→3:2→4:1) yielded the title compound (170 mg,71%). R_(f)=0.10 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.13.

Compounds of Type AL(rac.)-(1R*,5S*)-7-{4-[2-(2-Bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL1)

A sol. bicyclononene AK1 (540 mg, 0.61 mmol)I in CH₂Cl₂ (10 mL) wascooled to 0° C. HCl/dioxane (4M, 10 mL) was added and the ice bath wasremoved. After 4 h stirring at rt the solvents were removed underreduced pressure and the residue dried under high vacuum. The crude wasused without further purification.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethyl-ethyl ester hydrochloride salt (AL2)

As for compound AL1 but from bicyclononene AK2 (407 mg, 0.47 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06; ES+:796.34.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethyl-ethyl ester hydrochloride salt (AL3)

As for compound AL1 but from bicyclononene AK3 (570 mg, 0.65 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.04; ES+:766.34.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL4)

As for compound AL1 but from bicyclononene AK4 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.19; ES+:786.25.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL5)

As for compound AL1 but from bicyclononene AK5 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.18; ES+:782.28.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL6)

As for compound AL1 but from bicyclononene AK6 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.20.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL7)

As for compound AL1 but from bicyclononene AK7 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.21; ES+:778.30.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(4-methoxyphenoxymethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL8)

As for compound AL1 but from bicyclononene AK8 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.21.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3-methoxyphenoxymethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL9)

As for compound AL1 but from bicyclononene AK9 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.18.

(rac.)-(1R*,5S*)-6-(Cyclopropyl-m-tolyloxymethylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL10)

As for compound AL1 but from bicyclononene AKIO (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.24.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3,4-dimethylphenoxymethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL11)

As for compound AL1 but from bicyclononene AK11 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.28.

(rac.)-(1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL12)

As for compound AL1 but from bicyclononene AK12 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.18; ES+:778.30.

(rac.)-(1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL13)

As for compound AL1 but from bicyclononene AK13 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.21.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (AL14)

As for compound AL1 but from bicyclononene AK14 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.21.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL15)

As for compound AL1 but from bicyclononene AK15 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.18; ES+:796.28.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-tri-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL16)

As for compound AL1 but from bicyclononene AK16 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.21; ES+:794.30.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL17)

As for compound AL1 but from bicyclononene AK17 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.16.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-tri-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL18)

As for compound AL1 but from bicyclononene AK18 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.22; ES+:792.30.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL19)

As for compound AL1 but from bicyclononene AK19 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.01.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL20)

As for compound AL1 but from bicyclononene AK20 (about 0.55 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.26; ES+:806.26.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL21)

As for compound AL1 but from bicyclononene AK21 (519 mg, 0.54 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL22)

As for compound AL1 but from bicyclononene AK22 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.30; ES+:828.33.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL23)

As for compound AL1 but from bicyclononene AK23 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL).

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL24)

As for compound AL1 but from bicyclononene AK24 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.33; ES+:820.40.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL25)

As for compound AL1 but from bicyclononene AK25 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL26)

As for compound AL1 but from bicyclononene AK26 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.08; ES+:866.40.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL27)

As for compound AL1 but from bicyclononene AK27 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.07.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL28)

As for compound AL1 but from bicyclononene AK28 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08.

-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL29)

As for compound AL1 but from bicyclononene AK29 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.25; ES+:820.38.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL30)

As for compound AL1 but from bicyclononene AK30 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.35; ES+:854.30.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL31)

As for compound AL1 but from bicyclononene AK31 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.40; ES+:856.38.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL32)

As for compound AL1 but from bicyclononene AK32 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.28; ES+:838.40.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL33)

As for compound AL1 but from bicyclononene AK33 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.36; ES+:834.42.

1:1-Mixture of(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt and(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methyl-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-tri-chloro-1,1-dimethylethyl ester hydrochloride salt (AL34)

As for compound AL1 but from bicyclononenes AK34 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=0.99.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL35)

As for compound AL1 but from bicyclononene AK35 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.23; ES+:866.40.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL36)

As for compound AL1 but from bicyclononene AK36 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.59; ES+:834.42.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL37)

As for compound AL1 but from bicyclononene AK37 (about 0.8 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.01.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL38)

As for compound AL1 but from bicyclononene AK38 (312 mg, 0.35 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08; ES+:774.33.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[2-(2,3,6-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL39)

As for compound AL1 but from bicyclononene AK39 (340 mg, 0.40 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.05; ES+:740.42.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,6-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL40)

As for compound AL1 but from bicyclononene AK40 (374 mg, 0.43 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.07; ES+:762.34.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL41)

As for compound AL1 but from bicyclononene AK41 (350 mg, 0.41 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06; ES+:758.38.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL42)

As for compound AL1 but from bicyclononene AK42 (294 mg, 0.32 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL43)

As for compound AL1 but from bicyclononene AK43 (322 mg, 0.38 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08; ES+:752.39.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL44)

As for compound AL1 but from bicyclononene AK44 (159 mg, 0.18 mol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.07.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (AL45)

As for compound AL1 but from bicyclononene AK45 (237 mg, 0.26 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.00.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-n-tolyloxyethyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL46)

As for compound AL1 but from bicyclononene AK46 (185 mg, 0.21 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.09; ES+:784.40.

(rac.)-(1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,6-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL47)

As for compound AL1 but from bicyclononene AK47 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.09; ES+:754.44.

(rac.)-(1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL48)

As for compound AL1 but from bicyclononene AK48 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.10; ES+:788.41.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL49)

As for compound AL1 but from bicyclononene AK49 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.09; ES+:788.41.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL50)

As for compound AL1 but from bicyclononene AK50 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.09; ES+:772.41.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxy-licacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL51)

As for compound AL1 but from bicyclononene AK51 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.10; ES+:768.44.

1:1-Mixture of(rac.).-(1R*,5S*)-6-[((2*S)-2-hydroxy-2-phenylethyl)methyl-carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt and(rac.)-(1R*,5S*)-6-[((2S*)-2-hydroxy-2-phenylethyl)-methylcarbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL52)

As for compound AL1 but from bicyclononene AK52 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.02; ES+:744.44.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL53)

As for compound AL1 but from bicyclononene AK53 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.07.

(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[2-(2,3,6-tri-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL54)

As for compound AL1 but from bicyclononene AK54 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.10; ES+:768.44.

(rac.)-(1R*,5S*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[2-(2,3,6-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL55)

As for compound AL1 but from bicyclononene AK55 (about 0.3 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.03; ES+:784.44.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL56)

As for compound AL1 but from bicyclononene AK56 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08; ES+:785.26.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL57)

As for compound AL1 but from bicyclononene AK57 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL58)

As for compound AL1 but from bicyclononene AK58 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL59)

As for compound AL1 but from bicyclononene AK59 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL60)

As for compound AL1 but from bicyclononene AK60 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.07; ES+:788.40.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL61)

As for compound AL1 but from bicyclononene AK61 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL62)

As for compound AL1 but from bicyclononene AK62 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.07.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL63)

As for compound AL1 but from bicyclononene AK63 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL64)

As for compound AL1 but from bicyclononene AK64 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.07; ES+:788.39.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL65)

As for compound AL1 but from bicyclononene AK65 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL66)

As for compound AL1 but from bicyclononene AK66 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL67)

As for compound AL1 but from bicyclononene AK67 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (AL68)

As for compound AL1 but from bicyclononene AK68 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08.

1:1-Mixture of(rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[((2R*)2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethyl-ethyl ester hydrochloride salt and(rac.)-(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[((2S*)2-hydroxy-2-phenylethyl)methyl-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL69)

As for compound AL1 but from bicyclononene AK69 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=0.99; ES+:780.37.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL70)

As for compound AL1 but from bicyclononene AK70 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.06.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL71)

As for compound AL1 but from bicyclononene AK71 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.08.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

As for compound AL1 but from bicyclononene AK72 (about 0.5 mmol) inCH₂Cl₂ (5 mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.01.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[(2-chloro-benzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethyl-ethyl ester hydrochloride salt (AL73)

As for compound AL1 but from bicyclononene AK73 (0.28 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.98; ES+: 824.32.

(rac.)-(1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[2-(4-bromophenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL74)

As for compound AL1 but from bicyclononene AK74 (0.27 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=1.03; ES+: 792.36.

(rac.)-(1R,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[(2-chloro-benzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL75)

As for compound AL1 but from bicyclononene AK75 (0.22 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.92; ES+: 812.35.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL76)

As for compound AL1 but from bicyclononene AK76 (0.26 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.78; ES+: 808.40.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL77)

As for compound AL1 but from bicyclononene AK77 (0.29 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.97; ES+: 858.42.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL78)

As for compound AL1 but from bicyclononene AK78 (0.28 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.01; ES+: 804.42.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL79)

As for compound AL1 but from bicyclononene AK79 (0.2 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.03; ES+: 850.44.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL80)

As for compound AL1 but from bicyclononene AK80 (0.21 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.11; ES+: 848.43.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{[2-(2-chloro-phenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL81)

As for compound AL1 but from bicyclononene AK81 (0.27 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=5.09; ES+: 838.36.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL82)

As for compound AL1 but from bicyclononene AK82 (0.26 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.44; ES+: 840.42.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL83)

As for compound AL1 but from bicyclononene AK83 (0.24 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.89; ES+: 822.39.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL84)

As for compound AL1 but from bicyclononene AK84 (0.27 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL).

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL85)

As for compound AL1 but from bicyclononene AK85 (0.25 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.76; ES+: 850.40.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL86)

As for compound AL1 but from bicyclononene AK86 (0.27 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.99; ES+: 820.78.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt (AL87)

As for compound AL1 but from bicyclononene AK87 (0.18 mmol) in CH₂Cl₂ (5mL) and HCl/dioxane (4M, 5 mL). LC-MS: R_(t)=4.58; ES+: 834.43.

(rac.)-(1R*,5S*)-7-Hydroxy-9-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-benzyl ester 3-tert-butyl ester (AM)

Ti(OEt)₄ (2.92 mL, 13.9 mmol) was added to a sol. of bicyclononane A(13.0 g, 39.8 mmol) in benzyl alcohol (90 mL). The mixture was heated to125° C. and stirred at this temperature for 28 h. The mixture wasallowed to cool to rt and aq. 10% HCl (180 mL) was added. The mixturewas extracted with Et₂O (3×). The combined org. extracts were washedwith aq. NaHCO₃ (2×), with brine (1×). The org. extracts were then driedover MgSO₄, filtered, and the solvents were removed first under reducedpressure, then under high vacuum. Purification of the residue by FC(EtOAc/heptane 1:1→3:1→EtOAc) yielded the title compound (9.90 g, 64%).LC-MS: R_(t)=1.39; ES+: 389.25.

(rac.)-(1R*,5S*)-9-Methyl-7-trifluoromethanesulfonyloxy-3,9-diazabicyclo-[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-benzyl ester 3-tert-butyl ester (AN)

NaH (55% in oil, 2.20 g, 50.5 mmol) was added to a sol. of bicyclononaneAM (15.69 g, 40.4 mmol) in THF (290 mL) at 0° C. After 15 min. Tf₂NPh(19.2 g, 53.7 mmol) was added and the mixture was stirred overnightwhile warming up to rt. Ice was added and the mixture was diluted withEtOAc, and washed with aq. 10% Na₂CO₃. The org. extracts were dried overMgSO₄, filtered, and the solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane 1:1-3:1) yielded thetitle compound (17.1 g, 81%). R_(f)=0.15 (EtOAc/heptane 1:1). LC-MS:R_(t)=5.62; ES+: 521.37.

Compounds of Type AO(rac.)-(1R*,5S*)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-9-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-benzyl ester 3-tert-butyl ester (AO1)

BuLi (1.5M in hexane, 3.81 mL, 5.71 mmol) was added to a sol. of[3-(4-bromophenyl)propoxy]-tert-butyldimethylsilane (Kiesewetter D. O.,Tetrahedron Asymmetry, 1993, 4, 2183, 1.88 g, 5.71 mmol) in THF (33 mL)at −78° C. After 30 min ZnCl₂ (1M in THF, 6.97 mL, 6.97 mmol, preparedas described for compound G1) was added and the mixture was allowed towarm up to rt. Bicyclononene AN (1.65 g, 3.17 mmol) and Pd(PPh₃)₄ (92mg, 0.080 mmol) were added. The mixture was heated to 40° C. and stirredat this temperature for 30 min. The mixture was allowed to cool to rtand aq. 1M HCl (1 mL) was added.

The mixture was diluted with EtOAc and washed with aq. 1M NaOH (1×). Theorg. extracts were dried over MgSO₄, filtered, and the solvents wereremoved under reduced pressure. Purification of the residue by FC(MeOH/CH₂Cl₂ 1:49→3:97→2:48→5:95) yielded the title compound (1.78 g,90%). LC-MS: R_(t)=5.55; ES+: 681.30.

(rac.)-(1R*,5S*)-9-Methyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-benzyl ester 3-tert-butyl ester (AO2)

BuLi (1.6M in hexane, 19.40 mL, 31.0 mmol) was added to a sol. ofcompound C2 (9.90 g, 31.0 mmol) in THF (100 mL) at −78° C. After 30 minZnCl₂ (0.83M in THF, 43.8 mL, 37.2 mmol, prepared as described forcompound G1) was added and the mixture was allowed to warm up to rt.Bicyclononene AN (9.90 g, 19.0 mmol) and Pd(PPh₃)₄ (550 mg, 0.475 mmol)were added. The mixture was heated to reflux for 1 h. The mixture wasallowed to cool to rt and aq. 1M HCl (1 mL) was added. The mixture wasdiluted with EtOAc and washed with aq. 1M NaOH (1×). The org. extractswere dried over MgSO₄, filtered, and the solvents were removed underreduced pressure. Purification of the residue by FC (MeOH/CH₂Cl₂1:49→3:97→2:48→5:95) yielded the title compound (6.20 g, 54%). LC-MS:R_(t)=5.10; ES+: 611.59.

Compounds of Type AP(rac.)-(1R*,5S*)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 6-benzyl ester 3-tert-butyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AP1)

A sol. of bicyclononene AO1 (1.78 g, 2.87 mmol) and2,2,2-trichloro-tert-butyl chloroformate (3.44 g, 14.4 mmol) inCH₂ClCH₂Cl (35 mL) was heated to reflux for 2 h. The mixture was allowedto cool to rt and the solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane 1:8→1:1) yielded thetitle compound (1.88 g, 810%). LC-MS: R_(t)=8.34.

(rac.)-(1R*,5S*)-7-{4-[2-(2,3,5-Trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 6-benzyl ester 3-tert-butyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AP2)

As for compound AP1 but from bicyclononene AO2 (22.4 g, 36.7 mmol) and2,2,2-trichloro-tert-butyl chloroformate (44 g, 184 mmol) in CH₂ClCH₂Cl(400 mL). Purification of the residue by FC (EtOAc/heptane 1:8→1:1)yielded the title compound (19.2 g, 65%). LC-MS: R_(t)=7.95.

(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(3-hydroxypropyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-benzyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AQ)

HCl/dioxane (4M, 20 mL) was added to a sol. of bicyclononene AP1 (1.88g, 2.32 mmol) in CH₂Cl₂ (20 mL) was cooled to 0° C. The ice bath wasremoved and the mixture was stirred for 3 h at rt. The solvents wereremoved under reduced pressure and the residue was dried under highvacuum. This residue was then dissolved in THF (30 mL) and the sol. wascooled to −78° C. DMAP (cat. amount), DIPEA (1.60 mL, 9.28 mmol) andAcCl (0.165 mL, 2.32 mmol) were added. The mixture was stirred for 15min at −78° C. and MeOH(10 mL) was added. The mixture was allowed towarm up to rt, was dissolved in EtOAc and washed with aq. 1M HCl (1×)and aq. sat. NaHCO₃ (1×). The org. Extracts were dried over MgSO₄,filtered, and the solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane 1 . . .4→1:1→-EtOAc→MeOH/EtOAc 1:9) yielded the title compound (936 mg, 63%).LC-MS: R_(t)=5.47; ES+: 637.06.

Compounds of Type AR(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-benzyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AR1)

A mixture of bicyclononene AQ (468 mg, 0.73 mmol), 2,3,6-trifluorophenyl(216 mg, 1.46 mmol), azodicarboxylic dipiperidide (277 mg, 1.10 mmol)and tributyl phosphine (0.541 mL, 2.19 mmol) in toluene (15 mL) washeated to reflux for 20 h. The mixture was allowed to cool to rt and thesolvents were removed under reduced pressure. Purification of theresidue by FC (EtOAc/heptane 1:49→1:19→1:9) yielded the title compound(297 mg, 53%). LC-MS: R_(t)=6.87; ES+: 767.04.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-benzyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AR2)

As for the bicyclononene AR1, but from bicyclononene AQ1 (468 mg, 0.73mmol), 2-bromo-5-fluorophenol (0.163 mL, 1.46 mmol), azodicarboxylicdipiperidide (277 mg, 1.10 mmol) and tributyl phosphine (0.541 mL, 2.19mmol) in toluene (15 mL). Purification of the residue by FC(EtOAc/heptane 1:49→1:19→1:9) yielded the title compound (205 mg, 35%).LC-MS: R_(t)=7.06.

(rac.)-(1R*,5S*)-3-Acetyl-6-[(2-allylbenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (AS)

A mixture of bicyclononene AJ4 (225 mg, 0.300 mmol),(2-allylbenzyl)-cyclopropylamine (168 mg, 0.900 mmol), DIPEA (0.300 mL,1.80 mmol), DMAP (10 mg, 0.082 mmol), HOBt (41 mg, 0.300 mmol) andEDC.HCl (86 mg, 0.450 mmol) in CH₂Cl₂ (3 mL) was stirred for 2 days.EDC.HCl (29 mg, 0.150 mmol) was added again after 24 h and 30 h. Themixture was diluted with CH₂Cl₂ and washed with aq. 1M HCl (1×). Theorg. extracts were dried over MgSO₄, filtered, and the solvents wereremoved under reduced pressure. Purification of the residue by FC(EtOAc/heptane 1:4→3:7→2:3→1:1→3:2→7:3→4:1) yielded the title compound(185 mg, 67%). R_(f)=0.63 (EtOAc). LC-MS: R_(t)=7.40.

1:1-Mixture of(rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-((2R*)-2,3-dihydroxypropyl)benzyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester and(rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-((2S*)-2,3-dihydroxypropyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (AT)

A mixture of bicyclononene AS (281 mg, 0.316 mmol), NMO-H₂O (44.8 mg,0.332 mmol), and OsO₄ (2.5% in tert-BuOH, 0.0396 mL, 0.00316 mmol) inTHF (4 mL), tert-BuOH (2 mL) and water (1 mL) was stirred overnight.NMO-H₂O (10 mg, 0.074 mmol) and OsO₄ (0.010 mL, 0.008 mmol) were addedagain and the mixture was stirred again for 3 h. The solvents wereremoved under reduced pressure, and the residue was diluted with EtOAc,washed with aq. 1M HCl (1×), and with aq. sat. NaHCO3 (1×). The org.extracts were dried over MgSO₄, filtered, and the solvents were removedunder reduced pressure. Purification of the residue by FC (EtOAc/heptane1:4→2:3→3:2→4:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compounds (207mg, 71%). R_(f)=0.20 (EtOAc). LC-MS: R_(t)=6.23; ES+: 922.59.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2-oxoethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (AU)

A mixture of bicyclononenes AT (167 mg, 0.181 mmol) and NaIO₄ (40 mg,0.187 mmol) in THF (3 mL) and water (1 mL) was stirred at rt for 1 h.NaIO4 (20 mg, 0.01 mmol) was added again and the mixture was stirred for3 h. The mixture was diluted with EtOAc and washed with aq. sat. NaHCO₃(1×). The org. extracts were dried over MgSO₄, filtered, and thesolvents were removed under reduced pressure. The residue was driedunder high vacuum and the title compound (156 mg, 97%) was used withoutfurther purification. LC-MS: R_(t)=6.87; ES+: 891.78.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (AV)

A mixture of bicyclononene AU (44.6 mg, 0.05 mmol) and NaBH₄ (about 2mg, about 0.05 mmol) in MeOH (1 mL) was stirred at rt for 90 min. Themixture was diluted with EtOAc and washed with aq. 1M HCl (1×). The org.extracts were dried over MgSO₄, filtered and the solvents were removedunder reduced pressure. The residue was used without furtherpurification.

Compounds of Type AW(rac.)-(1R*,5S*)-7-[4-(3-Hydroxypropyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AW1)

TBAF (28.8 g, 91.4 mmol) was added to a sol. of bicyclononene H3 (45.6g, 60.9 mmol) in THF (900 mL) at 0° C. After 20 min, the ice bath wasremoved. After stirring the mixture at rt for 5 h, it was diluted withEtOAc and washed with water (2×). The org. extracts were dried overMgSO₄, filtered, and the solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane 1:4→1:1) yielded thetitle compound (27.6 g, 72%). R_(f)=0.22 (EtOAc/heptane 1:1). LC-MS:R_(t)=6.11; ES+: 655.23.

(rac.)-(1R*,5S*)-7-[4-(2-Hydroxyethoxy)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AW2)

As for compound AW1 but from bicyclononene H7 (44.4 g, 59.2 mmol) TBAF(28.0 g, 88.9 mmol) and THF (600 mL). Purification by FC (EtOAc/heptane1:3→1:1→EtOAc) yielded the title compound (23.67 g, 63%). R_(f)=0.20(EtOAc/heptane 1:1). LC-MS: R_(t)=6.02; ES+: 635.36. Compounds of typeAX

(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AX1)

A mixture of bicyclononene AW1 (20.22 g, 32.0 mmol),2,3,6-trifluorophenol (9.50 g, 64.0 mmol), azodicarboxylic dipiperidide(16.15 g, 64.0 mmol) and tributyl phosphine (85%, 27.9 mL, 96.0 mmol) intoluene (800 ml) was heated to reflux for 2 h. The mixture was allowedto cool to rt and the solvent removed under reduced pressure.Purification of the residue was purified by FC (EtOAc/heptane1:19→1:9→1:4) yielded the title compound (21.7 g, 89%). R_(f)=0.60(EtOAc/heptane 1:1). LC-MS: R_(t)=1.25; ES+: 765.22.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AX2)

As for AX1, but from bicyclononene AW1 (27.63 g, 43.6 mmol),2-bromo-5-fluorophenol (9.70 mL, 87.2 mmol), azodicarboxylicdipiperidide (22.0 g, 87.2 mmol), tributyl phosphine (32.2 mL, 131mmol), and toluene (550 ml). Purification of the residue by FC(EtOAc/heptane 1:19→1:9→1:4) yielded the title compound (31.67 g, 90%).R_(f)=0.60 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.63.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 6-ethyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AX3)

As for AX1, but from bicyclononene AW2 (11.83 g, 18.6 mmol),2-chloro-4,5-dimethylphenol (5.83 mL, 37.2 mmol), azodicarboxylicdipiperidide (9.39 g, 37.2 mmol), tributyl phosphine (85%, 16.2 mL, 55.8mmol), and toluene (300 ml). Purification of the residue by FC(EtOAc/heptane 1:19→1:9→1:3→1:1) yielded the title compound (13.35 g,93%). R_(f)=0.50 (EtOAc/heptane 1:1). LC-MS: R_(t)=7.60.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AX4)

As for AX1, but from bicyclononene AW2 (11.83 g, 18.6 mmol),4-bromophenol (6.43 mL, 37.2 mmol), azodicarboxylic dipiperidide (9.39g, 37.2 mmol), tributyl phosphine (85%, 16.2 mL, 55.8 mmol), and toluene(300 ml). Purification of the residue by FC (EtOAc/heptane1:19→1:9→1:3→1:1) yielded the title compound (13.6 g, 92%). R_(f)=0.50(EtOAc/heptane 1:1). LC-MS: R_(t)=7.49.

Compounds of Type AY(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AY1)

A mixture of bicyclononene AX1 (15.76 g, 20.7 mmol) in EtOH (600 mL) andaq. 1M NaOH (600 mL) was stirred for 7 h at 80° C. The mixture wasallowed to cool to rt and the solvents were partially removed underreduced pressure. The residue was diluted with EtOAc and aq. 1M HCl wasadded to pH 1-2. The phases were shaken, separated and the aq. phase wasextracted with EtOAc (2×). The combined org. extracts were dried overMgSO₄, filtered, and the solvents were removed under reduced pressure.Purification of the residue by FC (EtOAc/heptane 1:4→1:2→1:1) yieldedthe title compound (12.15 g, 80%). LC-MS: R_(t)=1.16; ES+: 737.21.

(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AY2)

As for compound AY1, but from bicyclononene AX2 (29.67 g, 36.8 mmol),EtOH (700 mL) and aq. 1M NaOH (700 mL). Purification by FC(EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compound26.67 g (94%). LC-MS: R_(t)=6.89; ES+: 749.92.

(rac.)-(1R*,5S*)-7-{4-[2-(2,3,5-Trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AY3)

Under N₂ Pd/C (10%, 1.92 g) was added to a sol. of bicyclononene AP2(19.2 g, 24.0 mmol) in MeOH (390 mL) cooled to 0° C. The mixture waspurged with H₂ (4×) and stirred at 0° C. under H₂ for 7 h. The mixturewas filtered through Celite, diluted with EtOAc and washed with aq. 1MHCl (1×). The org. extracts were dried over MgSO₄, filtered, and thesolvents were removed under reduced pressure. Purification by FC(EtOAc/heptane 1:3→1:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compound(4.26 g, 25%). LC-MS: R_(t)=7.10.

(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(AY4)

As for compound AY1, but from bicyclononene AX3 (13.35 g, 17.2 mmol),EtOH (670 mL) and aq. 1M NaOH (670 mL). Purification by FC(EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compound 12.3g (96%). R_(f)=0.75 (EtOAc). LC-MS: R_(t)=6.94.

(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AY5)

As for compound AY1, but from bicyclononene AX4 (13.6 g, 17.2 mmol),EtOH (680 mL) and aq. 1M NaOH (680 mL). Purification by FC(EtOAc/heptane 1:1→EtOAc→MeOH/EtOAc 1:9) yielded the title compound 12.2g (93%). R_(f)=0.75 (EtOAc). LC-MS: R_(t)=6.75.

Compounds of Type AZ(rac.)-(1R*,5S*)-3-Acetyl-7-[4-(3-hydroxypropyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (AZ1)

A mixture of bicyclononene S5 (3.23 g, 5.60 mmol) in EtOH (50 mL) andaq. 1M NaOH (50 mL) was stirred at 80° C. for 5 h. The mixture wasallowed to cool to rt and diluted with EtOAc. The mixture was brought topH 2 with aq. 1M HCl and extracted with EtOAc (3×). The combined org.extracts were dried over MgSO₄, filtered, and the solvents were removedunder reduced pressure. Purification by FC (MeOH/CH₂Cl₂ 1:19→1:9→1:4)yielded the title compound (1.40 g, 46%). LC-MS: R_(t)=0.89; ES+:547.28.

(rac.)-(1R*,5S*)-7-[4-(2-Hydroxyethyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(AZ2)

As for compound AZ1 but from bicyclononene H8 (4.96 g), EtOH (150 mL)and aq. 1M NaOH (150 mL). The crude material was used further withoutpurification.

Compounds of Type BA(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(tert-butyldimethylsilanyloxy)propyl]-phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (BA1)

A mixture of bicyclononene T4 (1.85 g, 2.79 mmol),(2-chlorobenzyl)-cyclopropylamine (1.52 g, 8.37 mmol), DMAP (85 mg, 0.70mmol), DIPEA (1.91 mL, 11.2 mmol), HOBt (377 mg, 2.79 mmol) and EDC-HCl(803 mg, 4.19 mmol) in CH₂Cl₂ (50 mL) was stirred at rt for 18 h. Themixture was diluted with more CH₂Cl₂ and washed with aq. 1M HCl (1×) andaq. sat. NaHCO₃ (1×). The org. extracts were dried over MgSO₄, filtered,and the solvents were removed under reduced pressure. Purification ofthe residue by FC (EtOAc/heptane 1:4→1:3→1:2→1:1) yielded the titlecompound (1.16 g, 50%). LC-MS: R_(t)=1.37.

(rac.)-(1R*,5S*)-7-{4-[2-(tert-Butyldiphenylsilanyloxy)ethyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester(BA2)

As for compound BA1, bur from bicyclononene T5 (crude, about 5.79 mmol),(2-chlorobenzyl)cyclopropylamine (3.10 g, 17.1 mmol), DIPEA (3.9 mL,22.8 mmol), DMAP (140 mg, 1.14 mmol), HOBt (770 mg, 5.70 mmol), andEDC-HCl (1.64 g, 8.55 mmol), in CH₂Cl₂ (50 mL). Purification of theresidue by FC (EtOAc/heptane 1:8→1:4) yielded the title compound 3.35 g(58%). R_(f)=0.55 (EtOAc/heptane 2:3). LC-MS: R_(t)=1.40.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(tert-butyldiphenylsilanyloxy)ethyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (BA3)

As for compound SI, from BA2 (1.45 g, 1.45 mmol), CH₂Cl₂ (10 mL), 4MHCl/dioxane (10 mL), THF (20 mL), without DMAP, DIPEA (4.62 mL, 27.0mmol), acetyl chloride (0.903 mL, 9.55 mmol), and MeOH (5 mL).Purification of the residue by FC (ErOAc/heptane 1:1→EtOAc→MeOH/EtOAc1:9) led to the title compound (1.34 g, 75%). R_(f)=0.30 (EtOAc/heptane1:1). LC-MS: R_(t)=1.39.

Compounds of Type BB(rac.)-(1R*,5S*)-3-Acetyl-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-[4-(3-hydroxypropyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (BB1)

A mixture of bicyclononene BA1 (1.16 g, 1.40 mmol) and TBAF (884 mg,2.80 mmol) in THF (10 mL) was stirred at rt for 90 min. The mixture wasdiluted with EtOAc and washed with water (2×) and brine (1×). The org.extracts were dried over MgSO₄, filtered, and the solvents were removedunder reduced pressure. Purification by FC (MeOH/CH₂Cl₂ 1:49→1:9)yielded the title compound (990 mg, 98%). R_(f)=0.47 (MeOH/CH₂Cl₂ 1:9).LC-MS: R_(t)=1.11.

(rac.)-(1R*,5S*)-3-Acetyl-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-[4-(2-hydroxyethyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester (BB2)

As for compound BB1, but from BA3 (1.99 g, 2.21 mmol), TBAF (1M in THF,4.5 mL, 4.5 mmol) in THF (15 mL). Purification by FC (EtOAc/heptane1:5→1:1→EtOAc) yielded the title compound (1.00 g, 68%). R_(f)=0.38(EtOAc/heptane 1:1). LC-MS: R_(t)=1.09; ES+: 698.02.

(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylicacid tert-butyl ester (BC)

Zn (1.63 g, 24.9 mmol) was added to a sol. of bicyclononene AK2 (2.25 g,2.50 mmol) in THF (30 mL) and AcOH (10 mL) under efficient stirring. Themixture was stirred efficiently for 2.5 h, then filtered and washed withTHF. The filtrate was diluted with EtOAc and washed with aq. 1M NaHO(2×). The org. extracts were dried over MgSO₄, and filtered. Evaporatingthe solvents under reduced pressure yielded the title compound that wasused without further purification.

(1R,5S)-9-Methyl-7-trifluoromethanesulfonyloxy-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-benzyl ester 3-tert-butyl ester (BD)

A sol. of bicyclononene AG (1.13 g; 2.91 mmol) in THF (8 ml) was addedto a suspension of NaH (ca 60%, 175 mg; 4.36 mmol) in THF (2 ml) at 0°C. After 30 min Tf₂NPh (1.56 g; 4.36 mmol) was added and the mixture wasstirred at rt for 12 h. Ice (5 g) was added and THF was evaporated. Theaq. residue was extracted with EtOAc (3×). The combine org. extractswere dried over MgSO₄, filtered, and the solvents were removed underreduced pressure. Purification of the residue by FC (EtOAc/cyclohexane1:1→EtOAc) yielded the title compound (1.28 g, 84%). R_(f)=0.53 (EtOAc).

(1R,5S)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-9-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-benzyl ester 3-tert-butyl ester (BE)

BuLi (1.6 M in hexane, 3.82 mL, 5.98 mmol) was added to a sol. of[3-(4-bromophenyl)propoxy]-tert-butyldimethylsilane (Kiesewetter D. O.,Tetrahedron Asymmetry, 1993, 4, 2183; 1.97 g; 5.98 mmol) in THF (4 ml)at −78° C. After 30 min, ZnCl₂ (1M in THF, 7.2 ml; 7.2 mmol) was addedand the mixture was allowed to warm up to rt. A sol. of bicyclononene BD(1.24 g: 2.39 mmol) in THF (7 ml) and Pd(PPh₃)₄ (69 mg; 0.060 mmol) wereadded after each other and the mixture was heated to 40° C. for 35 min.The reaction mixture was allowed to cool to rt, sat. solution of NH₄Clwas added, and the mixture was extracted with EtOAc (3×). The combinedorg. extracts were dried over MgSO₄, filtered, and the solvents wereremoved under reduced pressure. Purification of the residue by FC(EtOAc/cyclohexane 1:1→EtOAc) yielded the title compound (1.22 g, 82%).R_(f)=0.27 (EtOAc). LC-MS: R_(t)=5.68; ES+=621.30.

(1R,5S)-7-{4-[3-(tert-Butyldimethylsilanyloxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 6-benzyl ester 3-tert-butyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BF)

A mixture of bicyclononene BE (1.66 g, 2.67 mmol) andβ,β,β-trichloro-tert-butyl chloroformate (13.4 g, 240 mmol) in1,2-dichloroethane (10 ml) was heated to reflux for 4 h. The mixture wasallowed to cool to rt and the solvents were removed under reducedpressure. Purification of the residue by FC EtOAc/cyclohexane 1:4)yielded the title compound (1.75 g, 83%). R_(f)=0.43 (EtOAc/cyclohexane1:4). LC-MS: R_(t)=8.30.

(1R,5S)-7-[4-(3-Hydroxypropyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 6-benzyl ester 3-tert-butyl ester9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BH)

A sol. of bicyclononene BF (1.59 g, 1.96 mmol) in CH₂Cl₂ (3 ml) wascooled to 0° C. and HCl/dioxane (4M, 10 ml) was added. The mixture wasstirred for 2 h at 0° C. and subsequently for 3 h at rt. After thesolvents were removed under reduced pressure the crude was dried underhigh vacuum. The residue was dissolved in THF (5 ml). DMAP (12 mg, 0.098mmol) and DIPEA (1.34 ml; 7.849 mmol) were added and the mixture wascooled to −78° C. AcCl (0.153 ml; 2.16 mmol) was added and reactionmixture was stirred at −78° C. for 30 min. After addition of MeOH (1 ml)and warming-up to rt, aq. HCl (1M, 10 ml) was added and reaction mixturewas extracted with EtOAc (3×). The combined org. extracts were washedwith aq. sat. NaHCO₃ (1×), and the org. extracts were dried over MgSO₄,filtered, and the solvents were removed under reduced pressure.Purification of the residue by FC EtOAc/cyclohexane 1:3→1:1) yielded thetitle compound (280 mg, 22%). R_(f)=0.38 (EtOAc). LC-MS: R_(t)=5.43;ES+=637.17.

(1R,5S)-7-[4-(3-Hydroxypropyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-3,6,9-tricarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(BI)

A mixture of bicyclononene BH (140 mg; 0.219 mmol) and Pd/C (10%, 25 mg)in MeOH (4 ml) was stirred at rt under H₂ for 2 h. The mixture wasfiltered through Celite, washed with MeOH, and the solvents wereevaporated under reduced pressure. The crude product (110 mg) wasdirectly used in the next reaction without purification. R_(f)=0.15(EtOAc). LC-MS: R_(t)=4.41; ES−: 545.02.

(1R,5S)-7-[4-(3-Hydroxypropyl)phenyl]-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BJ)

A mixture of bicyclononene BI (95 mg; 0.17 mmol), phenethylmethylamine(0.48 ml; 0.34 mmol); HOBt (6.0 mg, 0.042 mmol), EDC.HCl (49 mg; 0.255mmol) and DMAP (5.0 mg; 0.042 mmol) in CHCl₃ (6 ml) was stirred at rtfor 14 h. Aq HCl (1M) was added and the mixture was extracted withCH₂Cl₂ (3×). The org. phase was washed with aq. sat. NaHCO₃ (1×), thecombined org. extracts were dried over MgSO₄, filtered, and the solventswere removed under reduced pressure. Purification of the residue by FC(EtOAc/cyclohexane 1:1→EtOAc) yielded the title compound (64 mg, 44%).R_(f)=0.25 (EtOAc). LC-MS: R_(t)=5.37; ES+: 664.29.

(1R,5S)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-ene-3,9-dicarboxylicacid 3-tert-butyl ester 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester(BK)

A mixture of bicyclononene BJ (60 mg; 0.090 mmol),2-bromo-5-fluorophenol (34 mg, 0.18 mmol), azodicarboxylic dipiperidide(34 mg; 0.135 mmol) and tributylphosphine (67 mg; 0.270 mmol) in toluene(2 ml) was heated to reflux for 20 h. The solvent was removed underreduced pressure. Purification of the residue was by FCEtOAc/cyclohexane 2:1→4:1) yielded the title compound (58 mg, 76%).R_(f)=0.60 (EtOAc). LC-MS: R_(t) 7.01; ES+=836.07.

(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BL)

HCl/dioxane (4M, 20 mL) was added to a sol. of bicyclononene AX2 (2.00g, 2.47 mmol) in CH₂Cl₂ (20 mL) cooled to 0° C. The ice bath removed andthe mixture was stirred at rt for 2 h. The solvents were removed underreduced pressure and the foamy residue dried under high vacuum. Amixture of this residue, DMAP (15 mg, 0.123 mmol) and DIPEA (1.69 mL,9.88 mmol) in THF (40 mL) was cooled to −78° C., and AcCl (0.186 mL,2.47 mmol) was added. The mixture was stirred for 20 min at −78° C. andMeOH (5 mL) was added. The mixture was allowed to warm up to rt, wasdiluted with EtOAc and washed with aq. 1M HCl (1×). The org. extractswere dried over MgSO₄, filtered, and the solvents were removed underreduced pressure. Purification of the residue by FC (EtOAc/heptane1:4→1:1→EtOAc) yielded the title compound (1.55 g, 83%). R_(f)=0.50(EtOAc).

Compounds of Type BM3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BM2)

Tributylphosphine (3.84 mL, 15.6 mmol) was added to a sol. ofbicyclononene S4 (3.00 g, 5.19 mmol), 2-bromo-5-fluorophenol (1.15 mL,10.4 mmol) and azodicarboxylic dipiperidide (1.97 g, 7.79 mmol) intoluene (30 mL). The mixture was heated to reflux for 2 h and allowed tocool to rt. The solvents were removed under reduced pressure.Purification by FC (EtOAc/heptane 1:1→2:1→3:1) yielded the titlecompound (2.70 g, 69%).

3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BM3)

As described for compound BM2, but from bicyclononene S4 (3.00 g, 5.19mmol), 2-chloro-4,5-dimethylphenol (1.64 g, 10.5 mmol), azodicarboxylicdipiperidide (1.98 g, 7.86 mmol), tributylphosphine (3.90 mL, 15.7 mmol)and toluene (50 mL). Purification by FC yielded the title compound (2.82g, 75%).

3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BM4)

As described for compound BM2, but from bicyclononene S4 (3.00 g, 5.19mmol), 2,6-dichloro-4-methylphenol (1.84 g, 10.38 mmol), azodicarboxylicdipiperidide (1.97 g, 7.79 mmol), tributylphosphine (3.84 mL, 15.6 mmol)and toluene (50 mL). Purification by FC yielded the title compound (2.76g, 72%).

3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BM5)

As described for compound BM2, but from bicyclononene S4 (3.20 g, 5.54mmol), 2,3-dichlorophenol (1.80 g, 11.1 mmol), azodicarboxylicdipiperidide (2.10 g, 8.31 mmol), tributylphosphine (4.11 mL, 16.6 mmol)and toluene (50 mL). Purification by FC yielded the title compound (2.22g, 55%).

3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BM7)

As described for compound BM2, but from bicyclononene S4 (3.00 g, 5.19mmol), 4-chloro-2-methylphenol (1.48 g, 10.4 mmol), azodicarboxylicdipiperidide (1.97 g, 7.79 mmol), tributylphosphine (3.84 mL, 15.6 mmol)and toluene (50 mL). Purification by FC yielded the title compound (1.36g, 37%).

3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BM9)

As described for compound BM2, but from bicyclononene S4 (3.00 g, 5.19mmol) 2,4,5-trichlorophenol (2.05 g, 10.4 mmol), azodicarboxylicdipiperidide (1.97 g, 7.79 mmol), tributylphosphine (3.84 mL, 15.6 mmol)and toluene (50 mL). Purification by FC yielded the title compound (2.76g, 72%).

3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-ethyl ester 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BM10)

As described for compound BM2, but from bicyclononene S4 (3.18 g, 5.50mmol) 2-chloro-5-fluorophenol (1.61 g, 11.0 mmol), azodicarboxylicdipiperidide (2.08 g, 8.25 mmol), tributylphosphine (4.10 mL, 16.6 mmol)and toluene (50 mL). Purification by FC yielded the title compound (2.67g, 69%).

Compounds of Type BN3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylic acid9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester (BN2)

A mixture of bicyclononene BM2 (2.69, 3.58 mmol) in aq. 1M NaOH (30 mL)and EtOH (70 mL) was stirred for 1 h at 85° C. The mixture was allowedto cool to rt and the solvents were partially removed under reducedpressure. The residue was acidified to pH 2 with aq. 1M HCl and thismixture was extracted with EtOAc (3×). The combined org. extracts weredried over MgSO₄, filtered, and the solvents were removed under reducedpressure. The crude title compound (2.96 g, quantitative yield) was usedfurther without purification.

3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester (BN3)

As described for compound BN2, but from bicyclononene BM3 (2.82 g, 3.94mmol), aq. 1M NaOH (30 mL) and EtOH (70 mL). The crude title compound(2.59 g, 96%) was used further without purification.

3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester (BN4)

As described for compound BN2, but from bicyclononene BM4 (2.75 g, 3.73mmol), aq. 1M NaOH (30 mL) and EtOH (70 mL). The crude title compound(2.63 g, quantitative yield) was used further without purification.

3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BN5)

As described for compound BN2, but from bicyclononene BM5 (2.22 g, 3.07mmol), aq. 1M NaOH (30 mL) and EtOH (70 mL). The crude title compound(1.59 g, 75%) was used further without purification.

3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethyl-ethyl) ester (BN7)

As described for compound BN2, but from bicyclononene BM7 (1.35 g, 1.92mmol), aq. 1M NaOH (30 mL) and EtOH (70 mL). The crude title compound(1.25 g, 97%) was used further without purification.

3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BN9)

As described for compound BN2, but from bicyclononene BM9 (2.31 g, 3.05mmol), aq. 1M NaOH (30 mL) and EtOH (70 mL). The crude title compound(2.19 g, 99%) was used further without purification.

3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6,9-dicarboxylicacid 9-(2,2,2-trichloro-1,1-dimethylethyl) ester (BN10)

As described for compound BN2, but from bicyclononene BM10 (2.82 g, 3.94mmol), aq. 1M NaOH (30 mL) and EtOH (70 mL). The crude title compound(1.90 g, 74%) was used further without purification.

Preparation of the Final Compounds Typical Procedure (A) for theAcylation:

To a solution of bicyclononene in anhydrous EtOAc was added vacuumdried-Amberlyst 21 (1.5 g/mmole of bicyclononene) or another suitablescavenger, followed by the addition of the desired acid chloride (1.5eq.). After shaking the suspension for 3 h, an aliquot water was addedand shaking was continued for 1 h. The resin was then removed byfiltration, washed with EtOAc and the filtrate was evaporated to yieldthe intermediate amide.

The synthesis of the sulfonamide, carbamate or urea derivatives wasperformed in analogy to the above-described procedure, by using thecorresponding sulfonyl chloride, chloroformate or carbamoyl chloriderespectively.

Typical Procedure (B) for Amide Formation from Acid Chlorides:

To a sol. of the acid chloride (1 eq.) in CH₂Cl₂ (2.5 mL/mmol) at 0° C.the amine (3 eq.) was added. The mixture was stirred for 3 h whilewarming up slowly to rt. If necessary, more CH₂Cl₂ was added, then thereaction mixture was washed with aq. sat. NaHCO₃ (1×) and aq. 1M HCl(1×). The extracts were dried over MgSO₄ and the solvents were removedunder reduced pressure. The obtained product was used without furtherpurification.

Typical Procedure (C) for an Amide Coupling with CDI

To a sol. of the carboxylic acid (1 eq.) in CH₂Cl₂ (4 mL/mmol) CDI (1eq.) was added. The sol. or suspension was stirred for 2 h at rt, thencooled to 0° C. The amine (6 eq.) was added and the sol. or suspensionwas stiffed for 2 h while warming up slowly to if. The sol. orsuspension was washed with water (1×). The org. extracts were evaporatedunder reduced pressure and the obtained residue was used further withoutpurification.

Typical Procedure (D) for the Reduction of an Amide to an Amine with LAH

To a sol. of the amide (1 eq.) was dissolved in THF (3 mL/mmol) LAH (1Min THF, 3 eq.) was added carefully. The mixture was stiffed at rt for 30min, then heated to 60° C. for 3 h before it was allowed to cool down toif, then to 0° C. For x g of LiAlH₄ initially added, was added x g ofwater, then x g of aq. 15% NaOH, and finally 3×g of water again. Theresulting mixture was stirred overnight, filtered, and the precipitatewashed with EtOAc. The filtrate was evaporated under reduced pressureand the residue diluted in a small amount of MeOH. The sol. was passedthrough a pad of SCX silica gel (sulfonic acid). Elution started withMeOH, followed by NH₃/MeOH. The amines eluted with the second secondeluent. The solvents were removed under reduced pressure. The isolatedamines were either used without further purification or purified byHPLC, depending on the purity.

Typical Procedure (E) for the Cleavage of the2,2,2-trichloro-1,1-dimethylethylcarbamate Protecting Group:

The crude product from another typical procedure was dissolved inTHF/AcOH (1:0.1) and treated with zinc (20 eq.). The suspension wasstirred for 5 h and filtered through celite, which was washed withEtOAc. The filtrate was evaporated under reduced pressure and theresidue was purified by HPLC.

Typical Procedure (F) for the Formation of Aryl Ether (MitsunobuReaction)

The bicyclononene (0.05 mmol) was dissolved or suspended in toluene(1.00 mL). The phenol derivative (0.075 mmol) in toluene (0.50 mL) wasadded. TMAD (0.075 mmol) in toluene (0.50 mL) was added, followed bytributylphosphine (0.15 mmol). The reaction mixture was stirred for 2 hat rt and then 2 h at 60° C. Sometimes, it was necessary to add a secondportion of tributylphosphine and to stir overnight. Sometimes, THF wasnecessary as cosolvent to dissolve the reactants. The reaction mixturewas allowed to cool to rt, then water was added. The mixture wasextracted with EtOAc, and the org. extracts were evaporated underreduced pressure.

Typical Procedure (G) for an Amide Coupling

To a sol. of bicyclononene (0.05 mmol) in CHCl₃ (2 mL) the desiredcarboxylic acid (0.10 mmol) was added. DIPEA (0.10 mmol), DMAP (0.01mmol), HOBt (0.01 mmol), and EDC.HCl (0.05 mmol) were added and thereaction mixture was stirred overnight. Sometimes, it was necessary toadd another portion of acid, DMAP, HOBt and EDC-HCl and to continuestirring for 24 h. CH₂Cl₂ was added and the mixture was washed withwater. The org. extracts were separated, dried over Na₂SO₄ and filtered.The solvent was removed under reduced pressure.

Typical Procedure (H) for an Amide Coupling

To a sol. of the bicyclononene (0.05 mmol) CHCl₃ or CH₂Cl₂ (2 mL) thedesired amine (commercially available or prepared following known,standard procedures) (0.10 mmol) was added. DIPEA (0.10 mmol), DMAP(0.01 mmol), HOBt (0.01 mmol) and EDC-HCl (0.05 mmol) were added. Thereaction mixture was stirred overnight. Sometimes, it was necessary toadd another portion of amine, DMAP, HOBt and EDC-HCl and to continuestirring the sol. for 24 h. CH₂Cl₂ was added and the mixture was washedwith water. The org. extracts were separated, dried over Na₂SO₄ andfiltered. The solvents were removed under reduced pressure.

Typical Procedure (J) for Reductive Amination

To a solution of aldehyde (1 eq.) in MeOH (0.5 mL/mmol) was added anamine (1.2 eq.). The solution was stirred for 2 h. Sodium borohydride(1.2 eq.) was added portionwise at 0° C. and then stirring wascontinued, at rt, for 4 h. A solution of NaOH 1N was added and the MeOHwas evaporated. The mixture was extracted with EtOAc twice and theorganic layer was washed with brine, dried over Na₂SO₄ and filtered. Thesolvent was removed under reduced pressure. The isolated amines wereeither used without further purification or purified by flashchromatography (EtOAc/heptane: 2/8), depending on the purity.

Typical Procedure (K) for an Anhydride Coupling

To a sol. of the bicyclononene (0.05 mmol) in CH₂Cl₂ (0.4 mL) was addedDIPEA (0.1 mmol) followed by the anhydride (0.06 mmol) in CH₂Cl₂ (0.4mL) at 0° C. After stirring for 3 h at rt, the solvent was evaporatedunder reduced pressure.

Typical Procedure (L) for Protecting Group (BOC and TBDMS) Cleavage

To a sol. of the bicyclononene (0.05 mmol) in CH₂Cl₂ (0.5 mL), cooled to0° C., was added 4M HCl/dioxane (0.5 mL) The ice bath was removed andthe solution was stirred for 1 h30 to 3 h, depending on the compound.The solvents were evaporated under reduced pressure without heating.

Typical Procedure (M) for the Saponification of Esters

A mixture of the ester (1 eq.) and LiOH (2 eq.) in THF was stirred at rtfor 2 h.

The solvents were removed under reduced pressure and the residue wasextracted on isolute sorbent (0.25 g pre-washed with 0.300 mL aq. 1MHCl, elution with 2 mL CH₂Cl₂). The solvent was removed under reducedpressure and the residue was used without further purification.

Preparation of Amines (2-Chlorobenzyl)cyclopropylamine

Synthesized according to typical procedures B and D from 2-chlorobenzoylchloride and cyclopropylamine.

Benzylcyclopropylamine

See Loeppky, R. N.; et al., J. Org. Chem., 2000, 65, 96.

(2-Chlorobenzyl)ethylamine

See Ishihara, Y; et al.; Chem. Pharm. Bull., 1991, 39, 3225.

Cyclopropyl-(3-trifluoromethylbenzyl)amine

See Brabander, H. J.; et al.; J. Org. Chem., 1967, 32, 4053.

Cyclopropylphenethylamine

See Smith, P. W.; et al.; J. Med. Chem., 1998, 41, 787.

Methyl(3-phenoxypropyl)amine

Synthesized according to typical procedures C and D from3-phenoxypropionic acid and methylamine.

(2-p-Tolyloxyethyl)methylamine

Synthesized according to typical procedures C and D from2-p-tolyloxyacetic acid and methylamine.

[2-(3-Chlorophenyl)ethyl]amine

Synthesized according to typical procedures C and D from3-chlorophenylacetic acid and methylamine.

[2-(2-Methoxyphenyl)ethyl]amine

Synthesized according to typical procedures C and D from2-methoxyphenylacetic acid and methylamine.

(2-Allylbenzyl)cyclopropylamine

BuLi (1.55 M in hexane, 14.7 mL, 22.7 mmol) was added to a sol. of1-bromo-2-(dimethoxymethyl)benzene (5.00 g, 21.6 mmol) in Et₂O (50 mL).The mixture was stirred for 30 min at −78° C. and MgBr₂.Et₂O (5.87 g,22.7 mmol) was added. The mixture was allowed to warm up to 0° C. over15 min and CuI (420 mg, 2.16 mmol) was added. The mixture was stirred at0° C. for 5 min and allyl bromide (1.92 mL, 22.7 mmol) was added. Themixture was stirred overnight while warming up to rt. Aq. 1M HCl (1 mL)was added and the mixture was diluted with Et₂O, and washed with aq. 1MHCl (1×). The org. Extracts were dried over MgSO₄, filtered, and thesolvents were removed under reduced pressure. The residue was dissolvedin acetone (20 mL) and water (10 mL), and TosOH (cat. amount) was added.The mixture was stirred for 5 h at rt, and the solvents were partiallyremoved under reduced pressure. The residue was diluted with Et₂O, andwashed with aq. 1M HCl (1×), and aq. sat. NaHCO₃ (1×). The org. extractswere dried over MgSO₄, filtered, and the solvents were removed underreduced pressure. Purification of the residue by FC (Et₂O/petroleumether 1:49→24:1) yielded 2-allylbenzaldehyde (1.06 g, 34%). Thiscompound was transformed into the title compound following typicalprocedure J with cyclopropylamine.

Cyclopropyl(2-fluorobenzyl)amine

Synthesized according to typical procedure J from 2-fluorobenzaldehydeand cyclopropylamine.

Cyclopropyl-(2-methylbenzyl)amine

Synthesized according to typical procedure J from 2-methylbenzaldehydeand cyclopropylamine.

Cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amine

Synthesized according to typical procedures C and D from(4-methoxyphenoxy)-acetic acid and cyclopropylamine.

Cyclopropyl-[2-(3-methoxyphenoxy)ethyl]amine

Synthesized according to typical procedures C and D from(3-methoxyphenoxy)-acetic acid and cyclopropylamine.

Cyclopropyl-(2-o-tolyloxyethyl)amine

Synthesized according to typical procedures C and D fromo-tolyloxyacetic acid and cyclopropylamine.

Cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amine

Synthesized according to typical procedures C and D from(3,4-dimethyl-phenoxy)acetic acid and cyclopropylamine.

[2-(2-Chlorophenyl)ethyl]cyclopropylamine

Synthesized according to typical procedures C and D from(2-chlorophenyl)-acetic acid and cyclopropylamine.

Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amine

Synthesized according to typical procedures C and D from(2,3-difluorophenyl)-acetic acid and cyclopropylamine.

Cyclopropyl-[2-(4-fluorophenyl)ethyl]amine

Synthesized according to typical procedures C and D from(4-fluorophenyl)acetic acid and cyclopropylamine.

Cyclopropyl-(2-o-tolylethyl)amine

Synthesized according to typical procedures C and D from o-tolylaceticacid and cyclopropylamine.

Cyclopropyl-(2-p-tolylethyl)amine

Synthesized according to typical procedures C and D from p-tolylaceticacid and cyclopropylamine.

Cyclopropyl-(3,5-dimethoxybenzyl)amine

Synthesized according to typical procedure J from2,5-dimethoxybenzaldehyde and cyclopropylamine.

(2-Chlorobenzyl)methylamine

See Kihara, M; et al.; Heterocycles, 1989, 29, 957.

(2-Chlorobenzyl)isopropylamine

Synthesized according to typical procedure J from 2-chlorobenzaldehydeand isopropylamine.

Cyclopropyl-(2-fluoro-5-methoxybenzyl)amine

Synthesized according to typical procedure J from2-fluoro-5-methoxybenzaldehyde and cyclopropylamine.

Cyclopropyl-(3-methoxybenzyl)amine

Synthesized according to typical procedure J from 3-methoxybenzaldehydeand cyclopropylamine.

Cyclopropyl-(3,4-dimethoxybenzyl)amine

Synthesized according to typical procedure J from3,4-dimethoxybenzaldehyde and cyclopropylamine.

(2-Chloro-3-trifluoromethylbenzyl)cyclopropylamine

Synthesized according to typical procedure J from2-chloro-3-trifluoromethylbenzaldehyde and cyclopropylamine.

(6-Chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine

Synthesized according to typical procedure J from6-chlorobenzo[1,3]dioxole-5-carbaldehyde and cyclopropylamine.

Cyclopropyl-(5-fluoro-2-methoxybenzyl)amine

Synthesized according to typical procedure J from5-fluoro-2-methoxybenzaldehyde and cyclopropylamine.

(2-Chloro-6-fluorobenzyl)cyclopropylamine

Synthesized according to typical procedure J from2-chloro-6-fluorobenzaldehyde and cyclopropylamine.

(2-Bromobenzyl)cyclopropylamine

Synthesized according to typical procedure J from 2-bromobenzaldehydeand cyclopropylamine.

Cyclopropyl-(2,6-difluorobenzyl)amine

Synthesized according to typical procedure J from2,6-difluorobenzaldehyde and cyclopropylamine.

Cyclopropyl-(2,3-dimethylbenzyl)amine

Synthesized according to typical procedure J from2,3-dimethylbenzaldehyde and cyclopropylamine.

Cyclopropyl-(3-fluoro-2-methylbenzyl)amine

Synthesized according to typical procedure J from3-fluoro-2-methylbenzaldehyde and cyclopropylamine.

Cyclopropyl-(3,5-difluorobenzyl)amine

Synthesized according to typical procedure J from3,5-difluorobenzaldehyde and cyclopropylamine.

(2-Chloro-3,6-difluorobenzyl)cyclopropylamine

Synthesized according to typical procedure J from2-chloro-3,6-difluorobenzaldehyde and cyclopropylamine.

(2,3-Dichlorobenzyl)cyclopropylamine

Synthesized according to typical procedure J from2,3-dichlorobenzaldehyde and cyclopropylamine.

Cyclopropyl-(3-trifluoromethoxybenzyl)amine

Synthesized according to typical procedure J from3-trifluoromethoxy-benzaldehyde and cyclopropylamine.

Cyclopropyl-(3-methylbenzyl)amine

Synthesized according to typical procedure J from 3-methylbenzaldehydeand cyclopropylamine.

Cyclopropyl-(2,3-difluorobenzyl)amine

Synthesized according to typical procedure J from2,3-difluorobenzaldehyde and cyclopropylamine.

(3-Chlorobenzyl)cyclopropylamine

Synthesized according to typical procedure J from 3-chlorobenzaldehydeand cyclopropylamine.

Cyclopropyl-(4-fluorobenzyl)amine

Synthesized according to typical procedure J from 4-fluorobenzaldehydeand cyclopropylamine.

Preparation of Other Reagents 4-Carbamoylbutyric acid

See Melnyk, O., et al.; J. Org. Chem., 2001, 66, 4153.

meso-3,4-Dihydroxytartaric acid anhydride

A mixture of meso-3,4-Diydroxytartaric acid (1.00 g, 6.67 mmol) andtrifluoroacetic acid anhydride (5 mL) was stirred for 2 h at rt. Thesolvents were removed under reduced pressure and the residue was used ascrude product without further purification.

Succinamic Acid

See Bellier, B., et al.; J. Med. Chem., 2000, 43, 3614.

SPECIFIC EXAMPLES Example 1 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester trifluoroacetate salt

Synthesized according to typical procedure A from bicyclononene N and4-chlorophenylacetyl chloride, then according to typical procedure E.LC-MS: R_(t)=4.57; ES+: 725.35.

Example 2 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyl-oxy)propoxy]phenyl}-3-(quinoxaline-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester trifluoroacetate salt

Synthesized according to typical procedure A from bicyclononene N and2-quinoxaloyl chloride, then according to typical procedure E. LC-MS:R_(t)=4.55; ES+: 728.94.

Example 3 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyl-oxy)propoxy]phenyl}-3-phenylmethanesulfonyl-3,9-diazabicyclo[3.3.1]-non-6-en-6-ylmethyl ester trifluoroacetate salt

Synthesized according to typical procedure A from bicyclononene N andphenylmethanesulfonyl chloride, then according to typical procedure E.LC-MS: R_(t)=4.75; ES+: 727.74.

Example 4 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyl-oxy)propoxy]phenyl}-3-(2-thiophen-2-ylacetyl)-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl ester trifluoroacetate salt

Synthesized according to typical procedure A from bicyclononene N andthiophen-2-ylacetyl chloride, then according to typical procedure E.LC-MS: R_(t)=4.52; ES+: 696.91.

Example 5 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-(benzo[b]thiophene-3-carbonyl)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-6-ylmethyl ester trifluoroacetate salt

Synthesized according to typical procedure A from bicyclononene N andbenzothiophene-3-carbonyl chloride, then according to typical procedureE. LC-MS: R_(t)=4.76; ES+: 733.80.

Example 6(rac.)-(1R*,5S*)-7-{4-[3-(2-Methoxybenzyloxy)propoxy]phenyl}-6-[2-(2-me-thoxyphenyl)acetoxymethyl]-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester trifluoroacetate salt

Prepared as compound N, but then purified by HPLC. LC-MS: R_(t)=5.30;ES+: 774.97.

Example 7(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]-methylamide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and [2-(2-chlorophenyl)ethyl]methylamine (Jaques B.; Wallace R. G.,Tetrahedron, 1977, 33, 581). LC-MS: R_(t)=0.89; ES+: 632.40.

Example 8 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxy-benzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoroacetate salt

Synthesized according to typical procedures A and E from bicyclononene Nand acetyl chloride. LC-MS: R_(t)=0.93; ES+: 615.29.

Example 9(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-methoxyphenyl)ethyl]-methylamide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and [2-(4-methoxyphenyl)ethyl]methylamine (Ho C. Y.; Kukla M. J.,Tetrahedron Lett. 1997, 38, 2799). LC-MS: R_(t)=0.83; ES+: 628.44.

Example 10 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{6-[3-(2-methoxybenzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]-non-6-en-6-ylmethylester trifluoroacetate salt

Synthesized according to typical procedures A and E from bicyclononene Pand 4-chlorophenylacetyl chloride. LC-MS: R_(t)=1.03; ES+: 726.44.

Example 11(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-chlorophenyl)ethyl]-methylamide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and [2-(4-chlorophenyl)ethyl]methylamine (You Q., et al., Chem. Res.Chin. Univ., 1992, 8, 468). LC-MS: R_(t)=0.90; ES+: 632.40.

Example 12(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(3-chlorophenyl)ethyl]-methylamide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and [2-(3-chlorophenyl)ethyl]methylamine. LC-MS: R_(t)=0.92; ES+:632.37.

Example 13(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid ethylphenethylamide tri-fluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and ethylphenethylamine (Cossy J., Rakotoarisoa, H., TetrahedronLett., 2000, 41, 2097). LC-MS: R_(t)=0.89; ES+: 612.46.

Example 14(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(3-methoxyphenyl)ethyl]-methylamide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and [2-(3-methoxyphenyl)ethyl]methylamine. LC-MS: R_(t)=0.88; ES+:628.41.

Example 15 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzy-loxy)propoxy]phenyl}-3-methyl-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoroacetate salt

A sol. of bicyclononene N (0.05 mmol) in CH₂Cl₂ (2 mL) was cooled to 0°C. DIPEA (0.10 mmol) and methyl iodide (0.10 mmol) were added. Themixture was stirred at 0° C. for 2 h, then overnight at rt. Methyliodide (0.50 mmol) and DIPEA (0.15 mmol) were added again and stirringwas continued for 4 h at rt. EtOAc was added and the mixture was washedwith water. The org. extracts were separated, dried over MgSO₄ andfiltered. The solvents were removed under reduced pressure and theresidue was processed further according to general procedure E. LC-MS:R_(t)=4.04; ES+: 587.38.

Example 16(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(3,4-dimethoxyphenyl)-ethyl]methylamide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and [2-(3,4-dimethoxyphenyl)ethyl]methylamine. LC-MS: R_(t)=0.89;ES+: 644.48.

Example 17 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyl-oxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester tri-fluoroacetate salt

Synthesized according to typical procedure E from bicyclononene N.LC-MS: R_(t)=0.83; ES+: 573.29.

Example 18(rac.)-N-((1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl)-2-(2-methoxyphenyl)-N-methyl-acetamidetrifluoroacetate salt

Synthesized according to typical procedures G and E from bicyclononene Zand (2-methoxyphenyl)acetic acid. LC-MS: R_(t)=3.98; ES+: 628.63.

Example 19(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl(3-phenylpropyl)amide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and N-methyl(3-phenylpropyl)amine (Lavastre I.; et al., Bull. Soc.Chim. Fr., 1995, 132, 188). LC-MS: R_(t)=0.88; ES+: 612.45.

Example 20(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-methoxyphenyl)ethyl]-methylamide trifluoroacetate

Synthesized according to typical procedures H and E from bicyclononeneT1 and [2-(2-methoxyphenyl]ethyl]methylamine. LC-MS: R_(t)=0.88; ES+:628.45.

Example 21(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylmethylamide trifluoro-acetate

Synthesized according to typical procedures H and E from bicyclononeneT1 and N-methylbenzylamine. LC-MS: R_(t)=0.84; ES+: 684.41.

Example 22 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoroacetate

Synthesized according to typical procedures F and E from bicyclononeneR2 and 2-chlorophenol. LC-MS: R_(t)=0.89; ES+: 589.34.

Example 23 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{6-[3-(2-methoxy-benzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoroacetate salt

Synthesized according to typical procedures A and E from bicyclononene Pand acetyl chloride. LC-MS: R_(t)=0.90; ES+: 616.44.

Example 24 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneR2 and 2-bromophenol. LC-MS: R_(t)=0.92; ES+: 633.26.

Example 25 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-[2-(4-chlorophenyl)ethyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-yl-methylester trifluoroacetate salt

To a sol. of bicyclononene N (0.05 mmol) in CH₂Cl₂ (2 mL) NaBH₃OAc(0.065 mmol) and (4-chlorophenyl)acetaldehyde (Zhuangyu Z., et al.,Synthesis, 1991, 539, 0.065 mmol) were added. The mixture was stirredovernight. The solvent was removed under reduced pressure and theresidue treated according to typical procedure E. LC-MS: R_(t)=4.88;ES+: 711.47.

Example 26 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{4-[2-(3-chloro-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneR1 and 3-chlorophenol. LC-MS: R_(t)=4.17; ES+: 575.62.

Example 27 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{4-[3-(3-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoro-acetate salt

Synthesized according to typical procedures F and E from bicyclononeneR2 and 3-chlorophenol. LC-MS: R_(t)=0.90; ES+: 589.33.

Example 28 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneR1 and 2-chlorophenol. LC-MS: R_(t)=0.94; ES+: 575.34.

Example 29(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid phenethylamide trifluoro-acetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and phenethylamine. LC-MS: R_(t)=0.91; ES+: 584.44.

Example 30 (rac.)-(2-Methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-[4-(3-phenoxy-propyl)phenyl]-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester trifluoro-acetate salt

Synthesized according to typical procedures F and E from bicyclononeneR2 and phenol. LC-MS: R_(t)=0.87; ES+: 555.31.

Example 31 1:1-Mixture of (2R)— and(2S)—N-((1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxyben-zyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl)-N-me-thyl-2-phenylpropionamidetrifluoroacetate salt

Synthesized according to typical procedures G and E from bicyclononene Zand (rac.)-2-phenylpropionic acid. LC-MS: R_(t)=0.87; ES+: 612.42.

Example 32(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-methoxyphenyl)ethyl]-amide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT1 and 2-(2-methoxyphenyl)ethylamine. LC-MS: R_(t)=4.06; ES+: 614.35.

Example 33(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-chlorophenol. LC-MS: R_(t)=0.84; ES+: 558.24.

Example 34(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-ethoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-ethoxyphenol. LC-MS: R_(t)=0.84; ES+: 568.30.

Example 35(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-acetylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-acetylphenol. LC-MS: R_(t)=1.13; ES+: 566.29.

Example 36(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-o-toluoxyethyl]phenyl}-3,9-diazabicyclo-[3.3.1]-non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-methylphenol. LC-MS: R_(t)=1.18; ES+: 538.27.

Example 37(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-methoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3-methoxyphenol. LC-MS: R_(t)=1.15; ES+: 554.28.

Example 38(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-trifluoromethoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3-trifluoromethoxyphenyl. LC-MS: R_(t)=1.19; ES+: 608.28.

Example 39(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-m-toluoxyethyl]phenyl}-3,9-diazabicyclo-[3.3.1]-non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3-methylphenol. LC-MS: R_(t)=1.17; ES+: 538.26.

Example 40(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-isopropylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3-isopropylphenol. LC-MS: R_(t)=1.19; ES+: 608.28.

Example 41(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diaz-bicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoro-acetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-chlorophenol. LC-MS: R_(t)=0.87; ES+: 572.13.

Example 42(rac.)—(R*,5S*)-3-Acetyl-7-{4-[3-(2-bromophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-bromophenol. LC-MS: R_(t)=0.79; ES+: 616.11.

Example 43(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-fluorophenol. LC-MS: R_(t)=0.75; ES+: 556.20.

Example 44(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-acetylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-acetylphenol. LC-MS: R_(t)=0.71; ES+: 580.20.

Example 45(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-o-toluoxypropyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-methylphenol. LC-MS: R_(t)=0.90; ES+: 552.20.

Example 46(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3-methoxyphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide tri-fluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3-methoxyphenol. LC-MS: R_(t)=0.86; ES+: 568.21.

Example 47(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-m-toluoxypropyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3-methylphenol. LC-MS: R_(t)=0.79; ES+: 552.21.

Example 48(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3-chlorophenol. LC-MS: R_(t)=4.44; ES+: 572.32.

Example 49(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-bromophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3-bromophenol. LC-MS: R_(t)=0.78; ES+: 602.10.

Example 50 (rac.)-(1R*,S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,3-dichlorophenol. LC-MS: R_(t)=0.78; ES+: 592.10.

Example 51(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-3-trifluoromethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-chloro-3-trifluoromethylphenol. LC-MS: R_(t)=0.80; ES+: 626.11.

Example 52(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,3-difluorophenol. LC-MS: R_(t)=0.74; ES+: 560.13.

Example 53(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,3-dimethylphenol. LC-MS: R_(t)=0.79; ES+: 559.19.

Example 54(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-ethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-ethylphenol. LC-MS: R_(t)=0.80; ES+: 552.19.

Example 55(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3-bromophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide tri-fluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3-bromophenol. LC-MS: R_(t)=0.92; ES+: 616.05.

Example 56(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide tri-fluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,3-dichlorophenol. LC-MS: R_(t)=0.93; ES+: 606.12.

Example 57(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chloro-3-trifluoromethylphenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-chloro-3-trifluoromethylphenol. LC-MS: R_(t)=0.93; ES+: 640.10.

Example 58(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide tri-fluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,3-difluorophenol. LC-MS: R_(t)=0.88; ES+: 574.17.

Example 59(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,3-dimethylphenol. LC-MS: R_(t)=0.93; ES+: 566.22.

Example 60(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-ethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoro-acetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-ethylphenol. LC-MS: R_(t)=0.93; ES+: 566.22.

Example 61(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-isopropylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-isopropylphenol. LC-MS: R_(t)=0.86; ES+: 580.22.

Example 62(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-tert-butylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-tert-butylphenol. LC-MS: R_(t)=0.89; ES+: 594.24.

Example 63(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(4-chloro-2-methoxyphenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 4-chloro-2-methoxyphenol. LC-MS: R_(t)=0.77; ES+: 602.14.

Example 64(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,4-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,4-dichlorophenol. LC-MS: R_(t)=0.84; ES+: 606.08.

Example 65(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(4-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 4-fluorophenol. LC-MS: R_(t)=0.76; ES+: 556.19.

Example 66(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-tert-butyl-4-methylphenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-tert-butyl-4-methylphenol. LC-MS: R_(t)=0.93; ES+: 608.25.

Example 67(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-bromo-5-fluorophenol. LC-MS: R_(t)=0.80; ES+: 634.05.

Example 68(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,5-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,5-difluorophenol. LC-MS: R_(t)=0.76; ES+: 574.14.

Example 69(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chloro-5-methylphenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-chloro-5-methylphenol. LC-MS: R_(t)=0.82; ES+: 586.16.

Example 70(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,5-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,5-dimethylphenol. LC-MS: R_(t)=0.83; ES+: 566.20.

Example 71(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-isopropylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-isopropylphenol. LC-MS: R_(t)=0.82; ES+: 566.22.

Example 72(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-tert-butylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-tert-butylphenol. LC-MS: R_(t)=0.85; ES+: 580.26.

Example 73(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-propionylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-propionylphenol. LC-MS: R_(t)=0.72; ES+: 580.21.

Example 74(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,4-dichlorophenol. LC-MS: R_(t)=0.80; ES+: 592.09.

Example 75(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-ter-butyl-4-methylphenoxy)ethyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-tert-butyl-4-methylphenol. LC-MS: R_(t)=0.88; ES+: 594.27.

Example 76(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-methoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 4-methoxyphenol. LC-MS: R_(t)=0.71; ES+: 554.18.

Example 77(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-bromo-5-fluorophenol. LC-MS: R_(t)=0.76; ES+: 620.09.

Example 78(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,5-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,5-difluorophenol. LC-MS: R_(t)=0.73; ES+: 560.17.

Example 79(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-chloro-5-methylphenol. LC-MS: R_(t)=0.78; ES+: 572.13.

Example 80(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-methoxy-5-methylphenoxy)ethyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-methoxy-5-methylphenol. LC-MS: R_(t)=0.72; ES+: 568.19.

Example 81(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,5-dimethylphenol. LC-MS: R_(t)=0.90; ES+: 552.24.

Example 82(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU1 and 2-(2-chlorophenoxy)ethanol. LC-MS: R_(t)=0.75; ES+: 574.15.

Example 83(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU1 and 2-(3-methylphenoxy)ethanol. LC-MS: R_(t)=0.76; ES+: 554.18.

Example 84(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chlorophenyl)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU1 and 2-(chlorophenyl)ethanol. LC-MS: R_(t)=0.77; ES+: 558.13.

Example 85(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-chlorophenyl)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU1 and 2-(3-chlorophyl)ethanol. LC-MS: R_(t)=0.77; ES+: 558.14.

Example 86(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-methoxyphenyl)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluo-roacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU1 and 2-(2-methoxyphyl)ethanol. LC-MS: R_(t)=0.85; ES+: 554.21.

Example 87(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,5-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,5-dichlorophenol. LC-MS: R_(t)=0.79; ES+: 592.07.

Example 88(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,6-trifluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,3,6-trifluorophenol. LC-MS: R_(t)=0.74; ES+: 578.14.

Example 89(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3,5-dimethylphenol. LC-MS: R_(t)=0.80; ES+: 552.20.

Example 90(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-chlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3-chlorophenol. LC-MS: R_(t)=0.77; ES+: 558.15.

Example 91(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3-trifluoromethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3-trifluoromethylphenol. LC-MS: R_(t)=0.78; ES+: 592.17.

Example 92(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-tert-butyl-2-methylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 4-tert-butyl-2-methylphenol. LC-MS: R_(t)=0.88; ES+: 594.22.

Example 93(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,4-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3,4-dichlorophenol. LC-MS: R_(t)=0.81; ES+: 592.12.

Example 94(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-bromo-3-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 4-bromo-3-methylphenol. LC-MS: R_(t)=0.81; ES+: 616.12.

Example 95(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,4-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3,4-dimethylphenol. LC-MS: R_(t)=0.78; ES+: 552.18.

Example 96(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,5-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3,5-dichlorophenol. LC-MS: R_(t)=0.82; ES+: 592.10.

Example 97(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3,5-dimethylphenol. LC-MS: R_(t)=0.79; ES+: 552.20.

Example 98(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,5-dimethoxyphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 3,5-dimethoxyphenol. LC-MS: R_(t)=0.72; ES+: 584.19.

Example 99(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2-dichloro-4,5-dimethylphenol. LC-MS: R_(t)=0.81; ES+: 586.17.

Example 100(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,3,5-trimethylphenol. LC-MS: R_(t)=0.82; ES+: 566.21.

Example 101(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,5-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,5-dichlorophenol. LC-MS: R_(t)=0.83; ES+: 606.12.

Example 102(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-acetyl-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-acetyl-5-fluorophenol. LC-MS: R_(t)=0.73; ES+: 598.18.

Example 103(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,3,6-trifluorophenol. LC-MS: R_(t)=0.88; ES+: 592.19.

Example 104(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,4-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,4-dimethylphenol. LC-MS: R_(t)=0.83; ES+: 566.22.

Example 105(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-tert-butyl-6-methylphenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-tert-butyl-6-methylphenol. LC-MS: R_(t)=0.88; ES+: 608.27.

Example 106(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(4-tert-butyl-2-methylphenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 4-tert-butyl-2-methylphenol. LC-MS: R_(t)=0.93; ES+: 608.25.

Example 107(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3,4-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3,4-dichlorophenol. LC-MS: R_(t)=0.84; ES+: 606.12.

Example 108(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(4-bromo-3-methylphenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 4-bromo-3-methylphenol. LC-MS: R_(t)=0.85; ES+: 630.11.

Example 109(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3,4-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3,4-dimethylphenol. LC-MS: R_(t)=0.82; ES+: 566.20.

Example 110(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3,5-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3,5-dichlorophenol. LC-MS: R_(t)=0.87; ES+: 606.13.

Example 111(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3,5-dimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 3,5-dimethylphenol. LC-MS: R_(t)=0.82; ES+: 566.21.

Example 112(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chloro-4,5-dimethylphenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2-chloro-4,5-dimethylphenol. LC-MS: R_(t)=0.85; ES+: 600.18.

Example 113(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,5-trimethylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU3 and 2,3,5-trimethylphenol. LC-MS: R_(t)=0.86; ES+: 580.23.

Example 114 (rac.)-Acetic acid(1R*,5S*)-2-(7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]methylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2-oxoethylester formate salt

Synthesized according to typical procedures A and E from bicyclononeneac and acetic acid chlorocarbonylmethyl ester. LC-MS: R_(t)=1.01; ES+:664.14.

Example 115(rac.)-(1R*,5S*)-7-{4-[3-(2-Chlorophenoxy)propyl]phenyl}-3-(2-cyanoacetyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]-methylamide formate salt

Synthesized according to typical procedures K and E from bicyclononeneac and cyanoacetic acid. LC-MS: R_(t)=1.02; ES+: 631.13.

Example 116(rac.)-(1R*,5S*)-3-(2-Acetylaminoacetyl)-7-{4-[3-(2-chlorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chloro-phenyl)ethyl]methylamide formate salt

Synthesized according to typical procedures K and E from bicyclononeneac and acetylaminoacetic acid. LC-MS: R_(t)=0.96; ES+: 663.14.

Example 117 1:1 Mixture of(1R,5S)-3-((4S)-2-acetylamino-4-methylpentanoyl)-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]methylamide formate salt and(1S,5R)-3-((4S)-2-acetyl-amino-4-methylpentanoyl)-7-{4-[3-(2-chlorophenoxy)propyl]phe-nyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)-ethyl]methylamide formate salt

Synthesized according to typical procedures K and E from bicyclononeneac and acetyl leucine. LC-MS: R_(t)=1.05; ES+: 719.19.

Example 118(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]-methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and [2-(2-chlorophenyl)ethyl]methylamine (Jaques B.; Wallace R. G.,Tetrahedron, 1977, 33, 581). LC-MS: R_(t)=0.90; ES+: 606.08.

Example 119(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-hydroxybenzyl)methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and 2-methylaminomethylphenol (Ross S. D., et al.; J. Org. Chem.,1966, 31, 133). LC-MS: R_(t)=0.83; ES+: 574.10.

Example 120(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t) 0.92; ES+: 617.94.

Example 121 1:1 Mixture of(rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid[(3R*)-3-(2-chloro-phenyl)butyl]methylamide formate salt and(rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [(3S*)-3-(2-chlorophenyl)butyl]methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and (rac.)-methyl(3-phenylbutyl)amine (Meyers A. I., et al; J. Am.Chem. Soc., 1982, 104, 877). LC-MS: R_(t)=0.91; ES+: 600.13.

Example 122(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl-(4-phenylbutyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and methyl(4-phenylbutyl)amine (Neale R. S., et al.; J. Org. Chem.,1965, 30, 3683). LC-MS: R_(t)=0.91; ES+: 600.20.

Example 123(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl-(3-phenoxypropyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and methyl(3-phenoxypropyl)amine. LC-MS: R_(t)=0.88; ES+: 602.09.

Example 124(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl-(4-phenylpentyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and methyl(5-phenylpentyl)amine (Neale R. S., et al.; J. Org. Chem.,1965, 30, 3683). LC-MS: R_(t)=0.95; ES+: 614.12.

Example 125(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-benzo[1,3]dioxol-5-ylpropyl)-methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and (3-benzo[1,3]dioxol-5-ylpropyl)methylamine (Dallacker, et al.;Chem. Ber., 1971, 104, 2517). LC-MS: R_(t)=0.86; ES+: 630.10.

Example 126(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-methoxyphenoxy)ethyl]-methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and [2-(4-methoxyphenoxy)ethyl]methylamine. LC-MS: R_(t)=0.84; ES+:618.03.

Example 127(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-chlorophenoxy)ethyl]-methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and [2-(4-chlorophenoxy)ethyl]methylamine. LC-MS: R_(t)=0.90; ES+:622.03.

Example 128(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl-(2-p-tolyloxyethyl)-amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and (2-p-tolyloxyethyl)methylamine. LC-MS: R_(t)=0.89; ES+: 602.08.

Example 129(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid diethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and diethylamine. LC-MS: R_(t)=0.79; ES+: 510.06.

Example 130(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl-(2-pyridin-2-ylethyl)-amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneT2 and ethyl(2-pyridin-2-ylethyl)amine. LC-MS: R_(t)=0.89; ES+: 602.08.

Example 131(1S,5R)-3-Acetyl-7-{4-[2-(2,3,6-trifluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide

Synthesized according to typical procedures F and E from bicyclononeneBJ and 2,3,6-trifluorophenol. LC-MS: R_(t)=0.94; ES+: 592.19. ee=80%.

Example 132 1:1-Mixture of(rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-((2R*)-2,3-dihydroxypropyl)benzyl]amidetrifluoroacetate salt and(rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-((2S*)-2,3-dihydroxypropyl)benzyl]amidetrifluoroacetate salt

Synthesized according to typical procedure E from bicyclononene AT.LC-MS: R_(t)=3.99; ES+: 720.49.

Example 133(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide trifluoroacetate salt

Synthesized according to typical procedure E from bicyclononene AV.LC-MS: R_(t)=3.94; ES+: 692.77.

Example 134(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylcyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and benzylcyclopropylamine. LC-MS: R_(t)=0.89 ES+: 646.41.

Example 135(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-ethylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.91 ES+: 668.44.

Example 136(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and (2-fluorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.90 ES+: 664.46.

Example 137(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methyl-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and (2-methylbenzyl)cyclopropylamine. LC-MS: R_(t)=0.92 ES+: 660.47.

Example 138(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and cyclopropyl[2-(4-methoxyphenoxy)ethyl]amine. LC-MS: R_(t)=0.90ES+: 706.44.

Example 139(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-m-tolyloxy-ethyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and cyclopropyl[2-(3-methylphenoxy)ethyl]amine. LC-MS: R_(t)=0.93ES+: 690.47.

Example 140(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and cyclopropyl[2-(3,4-dimethylphenoxy)ethyl]amine. LC-MS:R_(t)=0.94 ES+: 704.48.

Example 141(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropylphenethyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and cyclopropylphenethylamine. LC-MS: R_(t)=0.90 ES+: 660.50.

Example 142(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and [2-(2-chlorophenyl)ethyl]cyclopropylamine. LC-MS: R_(t)=0.92ES+: 694.44.

Example 143(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and [2-(2,3-difluorophenyl)ethyl]cyclopropylamine. LC-MS: R_(t)=0.91ES+: 696.47.

Example 144(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-fluoro-phenyl)ethyl]amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and [2-(4-fluorophenyl)ethyl]cyclopropylamine. LC-MS: R_(t)=0.91ES+: 678.53.

Example 145(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-O— tolylethyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and [2-(2-methylphenyl)ethyl]cyclopropylamine. LC-MS: R_(t)=0.92ES+: 674.55.

Example 146 1:1-Mixture of(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid ((2R*)-2-hydroxy-2-phenylethyl)methylamide formate salt and(rac.)-(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-3,9-diazabicycl-o[3.3.1]non-6-ene-6-carboxylicacid ((2S*)-2-hydroxy-2-phenylethyl)methyl-amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAJ4 and α-(methylaminomethyl)benzyl alcohol. LC-MS: R_(t)=0.85 ES+:650.49.

Example 147(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoro-methylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and (3-trifluoromethylbenzyl)cyclopropylamine. LC-MS: R_(t)=0.93ES+: 714.40.

Example 148(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-o-tolylethyl)-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ4 and [2-(2-methylphenyl)ethyl]cyclopropylamine. LC-MS: R_(t)=0.90ES+: 632.51.

Example 149(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide

Synthesized according to typical procedure E from bicyclononene AL2 andpurification by FC. LC-MS: R_(t)=0.84 ES+: 596.30.

Example 150(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL2 and glutaric anhydride. LC-MS: R_(t)=0.87 ES+: 710.42.

Example 151(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

Synthesized according to typical procedure L from bicyclononene AK2 and.LC-MS: R_(t)=1.06 ES+: 798.34.

Example 152(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

Synthesized according to typical procedure L from bicyclononene AK4 and.LC-MS: R_(t)=1.19 ES+: 788.25.

Example 153(rac.)-(1R*,5S*)-6-[(2-Fluorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

Synthesized according to typical procedure L from bicyclononene AK5.LC-MS: R_(t)=1.18 ES+: 784.27.

Example 154(rac.)-(1R*,5S*)-6-[(2-Methylbenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

Synthesized according to typical procedure L from bicyclononene AK7.LC-MS: R_(t)=1.21 ES+: 780.29.

Example 155(rac.)-(1R*,5S*)-6-[Cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

Synthesized according to typical procedure L from bicyclononene AK16.LC-MS: R_(t)=1.21 ES+: 794.30.

Example 156(rac.)-(1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

Synthesized according to typical procedure L from bicyclononene AK17.LC-MS: R_(t)=1.16.

Example 157(rac.)(1R*,5S)-6-[Cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid 2,2,2-trichloro-1,1-dimethylethyl ester hydrochloride salt

Synthesized according to typical procedure L from bicyclononene AK18.LC-MS: R_(t)=1.22 ES+: 794.30.

Example 158(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL2 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91 ES+: 738.52.

Example 159(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93 ES+:724.49.

Example 160 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt and (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL2 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.80 ES+:709.38.

Example 161(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL2 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86 ES+: 709.38.

Example 162(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzyl-cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL3 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.84 ES+: 675.49.

Example 163(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)ethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL4 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86 ES+: 697.40.

Example 164(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL5 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.85 ES+: 693.43.

Example 165(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethylbenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL6 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88 ES+: 743.41.

Example 166(rac.)-(1R*5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL7 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86 ES+: 689.47.

Example 167(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL8 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.85 ES+: 735.47.

Example 168(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(3-methoxyphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL9 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86 ES+: 735.47.

Example 169(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-m-tolyloxyethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL10 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87 ES+: 719.46.

Example 170(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL11 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.89 ES+: 733.49.

Example 171(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropylphenethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL12 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.85 ES+: 689.48.

Example 172(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chloro-phenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL13 and 4-carbamoylbutyric acid. LC-MS: R_(t) 0.87 ES+: 723.43.

Example 173(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL14 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86 ES+: 725.45.

Example 174(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-fluorophenyl)ethyl]amide

Synthesized according to typical procedures G and E from bicyclononeneAL15 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86 ES+: 707.44.

Example 175(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-o-tolylethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL16 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87 ES+: 703.47.

Example 176(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL17 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.85 ES+: 735.47.

Example 177(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL18 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87 ES+: 703.46.

Example 178 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylcyclopropylamide formate salt and (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzyl-cyclopropylamide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL3 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.78 ES+:675.47.

Example 179 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt and (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)ethylamide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL4 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.79 ES+:697.40.

Example 180 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt and (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL5 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.78 ES+:693.44.

Example 181 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethylbenzyl)amide formate salt and(1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethylbenzyl)amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL6 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.81 ES+:743.42.

Example 182 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt and (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylenzyl)amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL7 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.79 ES+:689.47.

Example 183 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-m-tolyloxyethyl)amide formate salt and (1S,5R)-3-((1R4S-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-m-tolyloxyethyl)amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL10 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.81 ES+:719.45.

Example 184 1:1-Mixture of(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt and(1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL17 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.78 ES+:735.48.

Example 185 1:1-Mixture of(1R,5S)-3-((1S,4R)-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)amide formate salt and(1S,5R)-3-((1S,4R)-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)-amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL18 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.81 ES+:703.48.

Example 186 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL2 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 726.40.

Example 187 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-(4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and (rac.)-(3S*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL3 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.84 ES+: 692.45

Example 188 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-tri-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL4 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 714.38

Example 189 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazbicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazbicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL5 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.84 ES+: 710.42

Example 190 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethyl-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL6 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 760.39

Example 191 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL7 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 706.44

Example 192 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL8 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.85 ES+: 752.43

Example 193 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxy-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3-methoxyphenoxy)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL9 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.85 ES+: 752.44

Example 194 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-m-tolyloxyethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(2-m-tolyloxyethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL10 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87 ES+: 736.45.

Example 195 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3,4-dimethyl-phenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL11 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.89 ES+: 750.47

Example 196 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-(6-(cyclopropylphenethyl-carbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-5-(6-(cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL12 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.85 ES+: 706.43

Example 197 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]-cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropyl-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL13 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87 ES+: 740.40

Example 198 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL14 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 742.42

Example 199 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL15 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 724.43.

Example 200 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-o-tolylethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL16 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87 ES+: 720.45

Example 201 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxy-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL17 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.85 ES+: 752.42

Example 202 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-p-tolylethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL18 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87 ES+: 720.43

Example 203(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylcyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL3 and acetyl chloride. LC-MS: R_(t)=0.88 ES+: 604.53

Example 204(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL4 and acetyl chloride. LC-MS: R_(t)=0.90 ES+: 626.48

Example 205(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl(2-fluorobenzyl)-amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL5 and acetyl chloride. LC-MS: R_(t)=0.89 ES+: 622.53

Example 206(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)-amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL7 and acetyl chloride. LC-MS: R_(t)=0.90 ES+: 618.54

Example 207(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl[2-(4-methoxy-phenoxy)ethyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL8 and acetyl chloride. LC-MS: R_(t)=0.89 ES+: 664.54

Example 208(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl[2-(3-methoxy-phenoxy)ethyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL9 and acetyl chloride. LC-MS: R_(t)=0.89 ES+: 664.53

Example 209(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl[2-(3-methyl-phenoxy)ethyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL10 and acetyl chloride. LC-MS: R_(t)=0.91 ES+: 648.53

Example 210(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropylphenethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL12 and acetyl chloride. LC-MS: R_(t)=0.89 ES+: 618.54

Example 211(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl(3,5-dimethoxy-benzyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL17 and acetyl chloride. LC-MS: R_(t)=0.88 ES+: 664.55

Example 212(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl(2-p-tolylethyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL18 and acetyl chloride. LC-MS: R_(t)=0.91 ES+: 632.54

Example 213(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopenta-noicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL3 and glutaric anhydride. LC-MS: R_(t)=0.86 ES+: 676.54

Example 214(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL4 and glutaric anhydride. LC-MS: R_(t)-0.88 ES+: 698.46

Example 215(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL5 and glutaric anhydride. LC-MS: R_(t)=0.86 ES+: 694.51

Example 216(rac.)-5-((1R*,5S*)-6-[Cyclopropyl(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL6 and glutaric anhydride. LC-MS: R_(t)=0.89 ES+: 744.51

Example 217(rac.)-5-((1R*,5S*)-6-[Cyclopropyl(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL7 and glutaric anhydride. LC-MS: R_(t)=0.88 ES+: 690.54

Example 218(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL8 and glutaric anhydride. LC-MS: R_(t)=0.87 ES+: 736.54

Example 219(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL9 and glutaric anhydride. LC-MS: R_(t)=0.87 ES+: 736.55

Example 220(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL10 and glutaric anhydride. LC-MS: R_(t)=0.89 ES+: 720.53

Example 221(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL11 and glutaric anhydride. LC-MS: R_(t)=0.90 ES+: 734.57

Example 222(rac.)-5-((1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL12 and glutaric anhydride. LC-MS: R_(t)=0.87 ES+: 690.52

Example 223(rac.)-5-((1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL13 and glutaric anhydride. LC-MS: R_(t)=0.89 ES+: 724.49

Example 224(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL14 and glutaric anhydride. LC-MS: R_(t)=0.88 ES+: 726.51

Example 225(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL15 and glutaric anhydride. LC-MS: R_(t)=0.87 ES+: 708.50

Example 226(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(2-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL16 and glutaric anhydride. LC-MS: R_(t)=0.88 ES+: 704.54

Example 227(rac.)-5-((1R*,5S*)-6-[Cyclopropyl(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL17 and glutaric anhydride. LC-MS: R_(t)=0.86 ES+: 736.55

Example 228(rac.)-5-((1R*,5S*)-6-[Cyclopropyl(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL18 and glutaric anhydride. LC-MS: R_(t)=0.88 ES+: 704.54

Example 229(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopen-tanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL3 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.91 ES+:690.55

Example 230(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL4 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.92 ES+:712.49

Example 231(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL5 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.91 ES+:708.51

Example 232(rac.)-5-((1R*,5S*)-6-[Cyclopropyl(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL6 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94 ES+:758.51

Example 233(rac.)-5-((1R*,5S*)-6-[Cyclopropyl(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL7 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.92 ES+:704.54

Example 234(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL8 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.92 ES+:750.54

Example 235(rac.)-5-((1R*,5S*)-6-(Cyclopropyl[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL9 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.92 ES+:750.56

Example 236(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL10 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93 ES+:734.58

Example 237(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(3,4-dimethylphenoxy)ethyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL11 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95 ES+:748.57

Example 238(rac.)-5-((1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL12 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.91 ES+:704.55

Example 239(rac.)-5-((1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL13 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93 ES+:738.53

Example 240(rac.)-5-(1R*,5S*)-6-{Cyclopropyl[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL14 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.92 ES+:740.54

Example 241(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL15 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.92 ES+:722.54

Example 242(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(2-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL16 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93 ES+:718.56

Example 243(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL17 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.91 ES+:750.55

Example 244(rac.)-5-((1R*,5S*)-6-{Cyclopropyl[2-(4-methylphenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL18 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93 ES+:718.56

Example 245(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL3 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.90 ES+: 704.53

Example 246(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL4 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91 ES+: 726.53

Example 247(rac.)-5-((1R*,5S*)-6-[Cylopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxo-pentanoicformate salt

Synthesized according to typical procedures K and E from bicyclononeneAL5 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.90 ES+: 722.54

Example 248(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL6 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93 ES+: 772.51

Example 249(rac.)-5-((1R*,5S*)-6-[Cylopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL7 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91 ES+: 718.57

Example 250(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL8 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.90 ES+: 764.55

Example 251(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL9 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.90 ES+: 764.54

Example 252(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL10 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92 ES+: 748.58

Example 253(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL11 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93 ES+: 762.58

Example 254(rac.)-5-((1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL12 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.90 ES+: 718.56

Example 255(rac.)-5-((1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL13 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92 ES+: 752.50

Example 256(rac.)-5-((1R*,5S*)-6-{[2-(2,3-Difluorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL14 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91 ES+: 754.53

Example 257 (rac.)-5-((1R*,5S*)-6-{[2-(4-Fluorophenyl)ethylcyclopropylcarbamoyl}-7-{-4-3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-30)yl)-2,2-dimethyl-5-oxopentanoic acid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL15 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91 ES+: 736.56

Example 258(rac.)-5-((1R*,5S*)-6-{[2-(2-Methylphenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL16 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92 ES+: 732.59

Example 259(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL17 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.90 ES+: 764.54

Example 260(rac.)-5-((1R*,5S*)-6-{[2-(4-Methylphenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL18 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92 ES+: 732.58

Example 261 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[(2-chlorobenzyl)ethyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL4 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.85 ES+:716.45

Example 262 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(2-fluoro-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL5 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.83 ES+:712.44

Example 263 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[Cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL6 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.87 ES+:762.42

Example 264 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methyl-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL7 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.85 ES+:708.46

Example 265 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL14 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.85 ES+:744.46

Example 266 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2-methyl-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(2-methylphenyl)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL16 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.86 ES+:722.52

Example 267 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxy-benzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL17 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.84 ES+:754.50

Example 268 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(4-methyl-phenyl)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-{cyclopropyl-[2-(4-methylphenyl)-ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL18 and meso-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.86 ES+:722.49

Example 269 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL38 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 700.52

Example 270 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethyl-carbamoyl]-7-{4-[3-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,5-tri-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL40 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 688.54

Example 271(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL37 and glutaric anhydride. LC-MS: R_(t)=0.86 ES+: 762.42

Example 272(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxo-pentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL37 and glutaric acid monomethyl ester chloride. LC-MS: R_(t)=0.88 ES+:776.43

Example 273(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL37 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.82 ES+: 761.45

Example 274(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxy-ethyl)benzyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL19 and acetyl chloride. LC-MS: R_(t)=0.84 ES+: 648.50

Example 275(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL19 and glutaric anhydride. LC-MS: R_(t)=0.85 ES+: 740.42

Example 276(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL19 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.87 ES+:734.52

Example 277(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL19 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.86 ES+: 748.52

Example 278(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL19 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.81; ES+: 719.52.

Example 279(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL22 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 740.38.

Example 280(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL23 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 736.41.

Example 281(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL24 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 736.38.

Example 282(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL25 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 732.45.

Example 283(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL26 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 778.41.

Example 284(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL27 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 762.42.

Example 285(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL28 and glutaric anhydride. LC-MS: R_(t)=0.92; ES+: 776.45.

Example 286(rac.)-5-[(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL29 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 732.44.

Example 287(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL30 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 766.35.

Example 288(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL31 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 768.35.

Example 289(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL32 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 750.40.

Example 290(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL33 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 746.43.

Example 291(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL35 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 778.40.

Example 292(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL36 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 746.43.

Example 293(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL22 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:754.37.

Example 294(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL23 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:750.39.

Example 295(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL24 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.96; ES+:801.40.

Example 296(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL25 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:746.43.

Example 297(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL26 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:793.40.

Example 298(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL27 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:776.41.

Example 299(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL28 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.97; ES+:791.40.

Example 300(rac.)-5-[(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL29 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:746.43.

Example 301(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL30 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:780.38.

Example 302(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL31 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:782.40.

Example 303(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL32 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:764.41.

Example 304(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester

Synthesized according to typical procedures A and E from bicyclononeneAL33 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:760.43.

Example 305(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL35 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:793.40.

Example 306(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL36 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:760.42.

Example 307(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-di-methyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL22 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 768.36.

Example 308(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL23 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: 764.39.

Example 309(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL24 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 815.40.

Example 310(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL25 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t) 0.93; ES+: 760.43.

Example 311(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL26 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: >805.

Example 312(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL27 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 790.47.

Example 313(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL28 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.95; ES+: 805.4.

Example 314(rac.)-5-[(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL29 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: 760.43.

Example 315(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL30 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 794.41.

Example 316(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL31 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 796.44.

Example 317(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL32 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 778.42.

Example 318(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL33 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 774.46.

Example 319(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL35 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: >805.

Example 320(rac.)-5-((1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL36 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 774.44.

Example 321 1:1-Mixture of(rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL22 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.87; ES+:758.33.

Example 322 1:1-Mixture of(rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL23 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.85; ES+:754.37.

Example 323 1:1-Mixture of(rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL24 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.89; ES+:805.4.

Example 324 1:1-Mixture of(rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL25 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.87; ES+:750.39.

Example 325 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL26 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.86; ES+:796.42.

Example 326 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL27 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.88; ES+:780.38.

Example 327 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)-ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL28 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.89; ES+:794.44.

Example 328 1:1-Mixture of(rac.)-(2R*,3S*)-4-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL29 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.86; ES+:750.36.

Example 329 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL30 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.88; ES+:784.34.

Example 330 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL32 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.85; ES+:768.34.

Example 331 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL33 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.88; ES+:764.41.

Example 332 1:1-Mixture of(rac.)-(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL35 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.86; ES+:797.38.

Example 333 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL36 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.87; ES+:764.38.

Example 334(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL22 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 739.49.

Example 335(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL23 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 735.50.

Example 336(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL25 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 731.55.

Example 337(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL26 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 777.52.

Example 338(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL28 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.90; ES+: 775.55.

Example 339(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL30 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.89; ES+: 765.46.

Example 340(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2,3-difluorophenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL31 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 767.48.

Example 341(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-fluorophenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL32 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 749.52.

Example 342(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-methylphenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL33 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.89; ES+: 745.54.

Example 343(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL35 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 777.53.

Example 344(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-methylphenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL36 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 745.54.

Example 345 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)ethylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL22 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87; ES+: 756.44.

Example 346 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL23 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86; ES+: 752.46.

Example 347 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL24 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.89; ES+: 803.40.

Example 348 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL25 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87; ES+: 748.52.

Example 349 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL26 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86; ES+: 794.40.

Example 350 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL27 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.89; ES+: 778.52.

Example 351 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL28 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.90; ES+: 792.42.

Example 352 1:1-Mixture of(rac.)-(3R*)-5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl]-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL29 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86; ES+: 748.50.

Example 353 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL30 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88; ES+: 782.49.

Example 354 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL31 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88; ES+: 784.53.

Example 355 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL32 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87; ES+: 766.47.

Example 356 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL33 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88; ES+: 762.55.

Example 357 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL35 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86; ES+: 794.38.

Example 358 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL36 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88; ES+: 762.55.

Example 359 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)-benzyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL19 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.81; ES+: 736.54.

Example 360(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures A and B from bicyclononeneAL38 and acetyl chloride. LC-MS: R_(t)=0.93; ES+: 612.52.

Example 361(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL40 and acetyl chloride. LC-MS: R_(t)=0.93; ES+: 600.50.

Example 362(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-fluorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL41 and acetyl chloride. LC-MS: R_(t)=0.91; ES+: 596.53.

Example 363(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-trifluoromethylbenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL42 and acetyl chloride. LC-MS: R_(t)=0.95; ES+: 646.54.

Example 364(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-methylbenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL43 and acetyl chloride. LC-MS: R_(t)=0.93; ES+: 592.56.

Example 365(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL44 and acetyl chloride. LC-MS: R_(t)=0.92; ES+: 638.58.

Example 366(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL38 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 684.54.

Example 367(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL39 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 650.57.

Example 368(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL40 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 672.55.

Example 369(rac.)-5-((1R*,5S*)-6-[(2-Fluorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL41 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 668.57.

Example 370(rac.)-5-((1R*,5S*)-6-[(3-Trifluoromethylbenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL42 and glutaric anhydride. LC-MS: R_(t)=0.92; ES+: 718.52.

Example 371(rac.)-5-((1R*,5S*)-6-[(2-Methylbenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL43 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 664.59.

Example 372(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{-4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL44 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 710.56.

Example 373(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL45 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 710.54.

Example 374(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL46 and glutaric anhydride. LC-MS: R_(t)=0.92; ES+: 694.57.

Example 375(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL40 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.96; ES+:686.54.

Example 376(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester

Synthesized according to typical procedures A and E from bicyclononeneAL41 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:682.57.

Example 377(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL43 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.96; ES+:678.61.

Example 378(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL38 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 712.51.

Example 379(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL39 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 678.60.

Example 380(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL40 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 700.52.

Example 381(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL41 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 696.57.

Example 382(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL43 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 692.60.

Example 383 1:1-Mixture of(rac.)-(3R*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(3S*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL43 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.87; ES+:682.57.

Example 384(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzyl-cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL39 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 649.59.

Example 385(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)ethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL40 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 671.56.

Example 386(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL41 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 667.6.

Example 387(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedure E from bicyclononene AK22.LC-MS: R_(t)=0.84; ES+: 628.36.

Example 3887-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK35.LC-MS: R_(t)=0.84; ES+: 666.43.

Example 3897-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK25.LC-MS: R_(t)=0.85; ES+: 618.41.

Example 3907-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]-non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide formate salt

Synthesized according to typical procedure E from bicyclononene AK26.LC-MS: R_(t)=0.84; ES+: 664.43.

Example 391 1:1-Mixture of(1R,5S)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt and(1S,5R)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy-licacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL35 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.80; ES+:777.50.

Example 392(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL20 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 752.43.

Example 393(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL20 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:766.42.

Example 394(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL20 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 780.46.

Example 395 1:1-Mixture of(rac.)-(3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL20 and meso-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.87; ES+:770.37.

Example 396(rac.)-5-{(1R*,5S*)-4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL20 and 4-carbamnoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 751.44.

Example 397(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL21 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 718.46.

Example 398(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL21 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:732.49.

Example 399 1:1-Mixture of(rac.)-(2R*,3S*)-4-((1R*,5S*)-6-(benzylcyclopropyl-carbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt and(rac.)-(2S*,3R*)-4-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL21 and (S,R)-2,3-dihydroxysuccinic anhydride. LC-MS: R_(t)=0.86; ES+:736.43.

Example 400(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylcyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL21 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 717.46.

Example 401 1:1-Mixture of(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt and(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL34 and glutaric anhydride. LC-MS: R_(t)=0.85; ES+: 722.46

Example 402 1:1-Mixture of(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt and(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL34 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.88; ES+:736.46

Example 403 1:1-Mixture of(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt and(rac.)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL34 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.88; ES+: 750.47

Example 404 1:1-Mixture of(rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxy-licacid ((2R*)-2-hydroxy-2-phenylethyl)methylamide formate salt and(rac.)-(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]-phenyl}-3-(4-carba-moylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid ((2R*)-2-hydroxy-2-phenylethyl)methylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL34 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.82; ES+: 721.46

Example 405 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)-propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL20 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 768.40

Example 406 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL21 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 734.47

Example 407(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]-cyclopropylamide formate salt

Synthesized according to typical procedure E from bicyclononene AK65.LC-MS: R_(t)=0.84; ES+: 620.45

Example 408(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxy-benzyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK70.LC-MS: R_(t)=0.84; ES+: 7632.32

Example 409(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(p-toluoyl-ethyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK71.LC-MS: R_(t)=0.85; ES+: 600.29

Example 410(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL73 and acetyl chloride. LC-MS: R_(t)=0.90; ES+: 664.33

Example 411(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-bromophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxy-benzyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL85 and acetyl chloride. LC-MS: R_(t)=0.88; ES+: 690.36

Example 412(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[(2-chloro-benzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL73 and glutaric anhydride. LC-MS: R_(t)=0.87; ES+: 736.31

Example 413(rac.)-5-((1R*,5S*)-6-(Benzylcyclopropylcarbamoyl)-7-{4-[2-(4-bromo-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopenta-noicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL74 and glutaric anhydride. LC-MS: R_(t)=0.85; ES+: 702.33

Example 414(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL76 and glutaric anhydride. LC-MS: R_(t)=0.86; ES+: 720.33

Example 415(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL77 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 770.27

Example 416(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL78 and glutaric anhydride. LC-MS: R_(t)=0.87; ES+: 716.34

Example 417(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl[2-(3,4-dimethylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL80 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 760.37

Example 418(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL81 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 750.31

Example 419(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL83 and glutaric anhydride. LC-MS: R_(t)=0.87; ES+: 734.34

Example 420(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL84 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 730.37

Example 421(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL85 and glutaric anhydride. LC-MS: R_(t)=0.86; ES+: 762.31

Example 422(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL86 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 730.37

Example 423(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL76 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.89; ES+: 748.35

Example 424(rac.)-5-((1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL81 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91; ES+: 778.33

Example 425(rac.)-5-((1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL82 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91; ES+: 780.36

Example 426(rac.)-5-((1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL84 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: 7758.39

Example 427(rac.)-5-{(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL85 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.89; ES+: 790.39

Example 428(rac.)-5-((1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL86 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91; ES+: 758.38

Example 429(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzyl-cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL74 and 4-carbamnoylbutyric acid. LC-MS: R_(t)=0.85; ES+: 735.34

Example 430(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-ethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL75 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.85; ES+: 723.32

Example 431(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL76 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.84; ES+: 719.33

Example 432(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL79 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.84; ES+: 761.34

Example 433(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chloro-phenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL81 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 749.32

Example 434(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL85 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.84; ES+: 761.35

Example 435(rac.)-(1R*,5S*)-7-{4-[2-(4-Bromophenoxy)ethoxy]phenyl}-3-(4-carbamoyl-butyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL87 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.80; ES+: 745.40

Example 436(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-formyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-ethylamide formate salt

Synthesized according to typical procedure E from bicyclononene AK57.Obtained as side-product after purification by HPLC. LC-MS: R_(t)=0.91;ES+: 622.25

Example 437(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-formyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-O— tolylethyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK68.Obtained as side-product after purification by HPLC. LC-MS: R_(t)=0.92;ES+: 628.31

Example 438(rac.)-(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-formyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK70.Obtained as side-product after purification by HPLC. LC-MS: R_(t)=0.90;ES+: 660.30

Example 439(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL56 and acetyl chloride. LC-MS: R_(t)=0.93; ES+: 648.37

Example 440(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-ethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL57 and acetyl chloride. LC-MS: R_(t)=0.92; ES+: 636.37

Example 441(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL58 and acetyl chloride. LC-MS: R_(t)=0.90; ES+: 632.41

Example 442(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL60 and acetyl chloride. LC-MS: R_(t)=0.91; ES+: 628.43

Example 443(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL70 and acetyl chloride. LC-MS: R_(t)=0.91; ES+: 674.44

Example 444(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL71 and acetyl chloride. LC-MS: R_(t)=0.92; ES+: 642.44

Example 445(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL56 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 720.36

Example 446(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL57 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 708.35

Example 447(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL58 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 704.37

Example 448(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL59 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 745.38

Example 449(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL60 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 700.41

Example 450(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL61 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 746.42

Example 451(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3-methoxyphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL62 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 746.41

Example 452(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL63 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 730.44

Example 453(rac.)-5-[(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL64 and glutaric anhydride. LC-MS: R_(t)=0.88; ES+: 700.41

Example 454(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropyl-carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL65 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 734.39

Example 455(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL66 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 736.41

Example 456(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL67 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 718.40

Example 457(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL68 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 714.43

Example 458(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL70 and glutaric anhydride. LC-MS: R_(t)=0.89; ES+: 746.41

Example 459(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methylphenyl)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL71 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 714.41

Example 460(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL56 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:734.37

Example 461(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL57 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:722.37

Example 462(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL58 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:718.40

Example 463(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL59 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.96; ES+:768.38

Example 464(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL60 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:714.43

Example 465(rac.)-5-[(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL64 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:714.41

Example 466(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL65 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:748.39

Example 467(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL66 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.94; ES+:750.40

Example 468(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL67 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:732.44

Example 469(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL68 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:728.45

Example 470(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL70 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.93; ES+:760.40

Example 471(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL71 and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:728.43

Example 472(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL56 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 748.40

Example 473(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL57 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 736.42

Example 474(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL58 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.91; ES+: 732.45

Example 475(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL60 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 728.48

Example 476(rac.)-5-[(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL64 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: 728.49

Example 477(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL65 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 762.42

Example 478(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL66 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 764.44

Example 479(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-fluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL67 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: 746.48

Example 480(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL68 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 742.51

Example 481(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL70 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.92; ES+: 774.45

Example 482(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL71 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 742.51

Example 483(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL56 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 719.43

Example 484(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL57 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 707.39

Example 485(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL58 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 703.43

Example 486(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethylbenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL59 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.89; ES+: 753.44

Example 487(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL60 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 699.47

Example 488(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL61 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 745.46

Example 489(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropylphenethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL64 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.86; ES+: 699.44

Example 490(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL65 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 733.42

Example 491(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL66 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 735.43

Example 492(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-fluorophenyl)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL67 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 717.43

Example 493(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-o-tolylethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL68 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 713.46

Example 494(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL70 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 745.45

Example 495(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL71 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 713.46

Example 496 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL56 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 736.43

Example 497 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethyl-carbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL57 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87 ES+: 724.40

Example 498 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL58 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 720.43

Example 499 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluoromethylbenzyl)-carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3-trifluormethylobenzyl)-carbamoyl]-3,9-diazabicycl-o[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL59 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.89 ES+: 770.40

Example 500 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-methoxyphenoxy)-ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL61 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 762.46

Example 501 1:1-Mixture of(rac.)-(3R*)-5-[(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-[(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL64 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.86 ES+: 716.46

Example 502 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL65 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 750.41

Example 503 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2,3-difluorophenyl)-ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL66 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 752.45

Example 504 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(4-fluorophenyl)ethyl]-carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL67 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87 ES+: 734.47

Example 505 1:1-Mixture of(rac.)-(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-9-yl)-3-hydroxy-5-oxo-pentanoicacid formate salt and(rac.)-(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-9-yl)-3-hydroxy-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene BC and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88; ES+: 726.32

Example 506(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneBC and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.95; ES+: 738.37

Example 507(rac.)-4-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-4-oxo-butyricacid

Synthesized according to typical procedures K and E from bicyclononeneBC and succinic anhydride. LC-MS: R_(t)=0.90; ES+: 696.32

Example 508(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylicacid 6-[(2-chlorobenzyl)cyclopropyl-amide]9-dimethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and dimethylcarbamoyl chloride. LC-MS: R_(t)=0.94; ES+: 667.38

Example 509(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and methyl chloroformate. LC-MS: R_(t)=0.96; ES+: 654.34

Example 510(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylicacid ethyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and ethyl chloroformate. LC-MS: R_(t)=0.98; ES+: 668.37

Example 511(rac.)-3-[(1R*,5S*)-(6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)amino]propionicacid ethyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and ethyl 4-isocyanatopropionate. LC-MS: R_(t)=0.95; ES+: 739.36

Example 512 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-o-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid

Synthesized according to typical procedures K, E and L frombicyclononene AL68 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 730.49

Example 513 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL70 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.87; ES+: 762.47

Example 514 1:1-Mixture of(rac.)-(3R*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt and(rac.)-(3S*)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-6-[cyclopropyl(2-p-tolylethyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-3-hydroxy-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K, E and L frombicyclononene AL71 and 3-(tert-butyldimethylsilyloxy)glutaric anhydride.LC-MS: R_(t)=0.88 ES+: 730.49

Example 515 1:1-Mixture of(1R,5S)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt and(1S,5R)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL56 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.81; ES+:791.37

Example 516 1:1-Mixture of(1R,5S)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt and(1S,5R)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3-((2S,4R)-4-hydroxypyrrolidine-2-carbonyl)-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt

Synthesized according to typical procedures G, E and L frombicyclononene AL60 and BOC-L-hydroxyproline. LC-MS: R_(t)=0.81; ES+:699.45

Example 517(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropylphenethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL47 and acetyl chloride. LC-MS: R_(t)=0.92; ES+: 592.52

Example 518(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL48 and acetyl chloride. LC-MS: R_(t)=0.94; ES+: 626.51

Example 519(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL49 and acetyl chloride. LC-MS: R_(t)=0.93; ES+: 628.54

Example 520(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxy-benzyl)amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL53 and acetyl chloride. LC-MS: R_(t)=0.92; ES+: 638.54

Example 521(rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-Trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)-amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL54 and acetyl chloride. LC-MS: R_(t)=0.94; ES+: 606.54

Example 522(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxy-ethyl)benzyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL55 and acetyl chloride. LC-MS: R_(t)=0.87; ES+: 622.55

Example 523(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL72 and acetyl chloride. LC-MS: R_(t)=0.85; ES+: 658.47

Example 524(rac.)-5-((1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL47 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 664.56

Example 525(rac.)-5-((1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL48 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 698.45

Example 526(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid

Synthesized according to typical procedures K and E from bicyclononeneAL49 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 700.50

Example 527(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{-4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL50 and glutaric anhydride. LC-MS: R_(t)=0.90; ES+: 682.54

Example 528(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid

Synthesized according to typical procedures K and E from bicyclononeneAL51 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 678.55

Example 529 1:1-Mixture of(rac.)-5-((1R*,5S*)-6-[cyclopropyl-((2R*)-2-hydroxy-2-phenylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt and(rac.)-5-((1R*,5S*)-6-[cyclopropyl-((2S*)-2-hydroxy-2-phenylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL52 and glutaric anhydride. LC-MS: R_(t)=0.85; ES+: 654.50

Example 530(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL53 and glutaric anhydride. LC-MS: R_(t)=0.879; ES+: 710.50

Example 531(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL54 and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 678.56

Example 532(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid

Synthesized according to typical procedures K and E from bicyclononeneAL55 and glutaric anhydride. LC-MS: R_(t)=0.85; ES+: 694.53

Example 533(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL72 and glutaric anhydride. LC-MS: R_(t)=0.84; ES+: 730.46

Example 534(rac.)-5-((1R*,5S*)-6-(Cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,5-tri-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-di-methyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL47 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 692.55

Example 535(rac.)-5-((1R*,5S*)-6-{[2-(2-Chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL48 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.95; ES+: 726.48

Example 536(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(2,3-difluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL49 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 728.51

Example 537(rac.)-5-((1R*,5S*)-6-{Cyclopropyl-[2-(4-fluorophenyl)ethyl]carbamoyl}-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL50 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.94; ES+: 710.51

Example 538(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-o-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL51 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.95; ES+: 706.54

Example 539(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL53 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.93; ES+: 738.55

Example 540(rac.)-5-((1R*,5S*)-6-[Cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL54 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.95; ES+: 706.53

Example 541(rac.)-5-((1R*,5S*)-7-{4-[2-(2-Chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]-non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL72 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.87; ES+: 758.46

Example 542(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-phenethylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL47 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 663.55

Example 543(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chloro-phenyl)ethyl]cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL48 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.90; ES+: 697.49

Example 544(rac.)-(1R*,5S*)-3-(4-Carbamoylbutryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2,3-difluorophenyl)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL49 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.89; ES+: 699.49

Example 545(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-fluorophenyl)ethyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL50 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 681.54

Example 546(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyrl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL53 and 4-carbamnoylbutyric acid. LC-MS: R_(t)=0.87; ES+: 709.50

Example 547(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyrl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL54 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.89; ES+: 677.57

Example 548(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,5-trimethylphenoxy)-ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL55 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.83; ES+: 693.53

Example 549(rac.)-(1R*,5S*)-3-(4-Carbamoylbutyryl)-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2-hydroxyethyl)benzyl]amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL72 and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.82; ES+: 729.48

Example 550 (rac.)-Acetic acid(1R*,5S*)-2-(2-{[(3-acetyl-7-{4-[2-(2,3,5-trimethyl-phenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbonyl)cyclopropylamino]methyl}phenyl)ethylester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL and acetyl chloride. LC-MS: R_(t)=0.93; ES+: 664.55

Example 551 (rac.)-Acetic acid(1R*,5S*)-2-(2-{[(3-acetyl-7-{4-[2-(2-chloro-4,5-dimethyl-phenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbonyl)cyclopropylamino]methyl}phenyl)ethylester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL72 and acetyl chloride. LC-MS: R_(t)=0.91; ES+: 700.44

Example 552(rac.)-(1R*,5S*)-7-{4-[2-(2,3,5-Trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-fluorophenyl)-ethyl]amide formate salt

Synthesized according to typical procedure E from bicyclononene AK50.LC-MS: R_(t)=0.86; ES+: 568.50

Example 553(rac.)-(1R*,5S*)-7-{4-[2-(2,3,5-Trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)-amide formate salt

Synthesized according to typical procedure E from bicyclononene AK53.LC-MS: R_(t)=0.85; ES+: 596.53

Example 554 (rac.)-Acetic acid(1R*,5S*)-2-(2-{[(3-acetyl-7-{4-[2-(4-bromophenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carbonyl)cyclopropyl-amino]methyl}phenyl)ethylester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL87 and acetyl chloride. LC-MS: R_(t)=0.89; ES+: 716.35

Example 555 1:1 Mixture of(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[((2R*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt and(rac.)-5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-6-[((2S*)-2-hydroxy-2-phenylethyl)methylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL69 and 2,2-dimethylglutaric anhydride. LC-MS: R_(t)=0.88; ES+: 718.47

Example 556(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL20 and acetyl chloride. LC-MS: R_(t)=3.63; ES+: 680.28.

Example 557(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylcyclopropylamide formate salt

Synthesized according to typical procedure E from bicyclononene AK3.LC-MS: R_(t)=0.83; ES+: 562.38

Example 558(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedure E from bicyclononene AK4.LC-MS: R_(t)=0.84; ES+: 584.35

Example 559(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK5.LC-MS: R_(t)=0.83; ES+: 580.38

Example 560(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethyl-benzyl)amide

Synthesized according to typical procedure E from bicyclononene AK6.LC-MS: R_(t)=0.86; ES+: 630.43

Example 561(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK7.LC-MS: R_(t)=0.84; ES+: 576.42

Example 562(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(4-methoxy-phenoxy)ethyl]amide formate salt

Synthesized according to typical procedure E from bicyclononene AK8.LC-MS: R_(t)=0.83; ES+: 622.45

Example 563(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]-cyclopropylamide formate salt

Synthesized according to typical procedure E from bicyclononene AK13.LC-MS: R_(t)=0.86; ES+: 610.39

Example 564(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-[2-(2,3-difluoro-phenyl)ethyl]amide formate salt

Synthesized according to typical procedure E from bicyclononene AK14.LC-MS: R_(t)=0.85; ES+: 612.44

Example 565(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-o-tolylethyl)amide formate salt

Synthesized according to typical procedure E from bicyclononene AK16.LC-MS: R_(t)=0.85; ES+: 590.42

Example 566(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-p-tolylethyl)amide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAK18. LC-MS: R_(t)=0.85; ES+: 590.42

Example 567(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,5-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB1 and 2,5-difluorophenol. LC-MS: R_(t)=0.89; ES+: 614.40

Example 568(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB1 and 2,3-dichlorophenol. LC-MS: R_(t)=0.94; ES+: 654.32

Example 569(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chloro-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB1 and 2-chloro-5-fluorophenol. LC-MS: R_(t) 0.93; ES+: 636.36

Example 570(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3-cyanopyridin-2-yloxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB1 and 2-hydroxynicotinonitrile. LC-MS: R_(t)=0.86; ES+: 610.42

Example 571(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-[(2-chlorobenzyl)cyclopropyl-amide]3-dimethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and dimethylcarbamoyl chloride. LC-MS: R_(t)=0.91; ES+: 667.42

Example 572(rac.)-(1R*,5S*)-7-{4-[3-(2,3,6-Trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-[(2-chlorobenzyl)cyclopropyl-amide]3-diethylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and diethylcarbamoyl chloride. LC-MS: R_(t)=0.95; ES+: 695.44

Example 573(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and methyl chloroformate. LC-MS: R_(t)=0.91; ES+: 654.37

Example 574(rac.)-(1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylicacid ethyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and ethyl chloroformate. LC-MS: R_(t)=0.93; ES+: 668.40

Example 575(rac.)-(1R*,5S*)-3-Methanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and methylsulfonyl chloride. LC-MS: R_(t)=0.92; ES+: 674.37

Example 576(rac.)-(1R*,5S*)-3-Ethanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and ethylsulfonyl chloride. LC-MS: R_(t)=0.93; ES+: 688.36

Example 577(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid ethyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and glutaric acid monoethylester chloride. LC-MS: R_(t)=0.94; ES+:738.41

Example 578(rac.)-4-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-4-oxo-butyricacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneAL2 and succinic anhydride. LC-MS: R_(t)=0.87 ES+: 696.36

Example 579(rac.)-3-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)amino]propionicacid ethyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and ethyl 4-isocyanatopropionate. LC-MS: R_(t)=0.93; ES+: 739.41

Example 580(rac.)4-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)amino]butyricacid ethyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneAL2 and ethyl 4-isocyanatobutyrate. LC-MS: R_(t)=0.93; ES+: 753.39

Example 581(rac.)-(1R*,5S*)-3-(3-Carbamoylpropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL2 and succinamic acid. LC-MS: R_(t)=0.85; ES+: 695.38

Example 582(rac.)-(1R*,5S*)-3-(2-Hydroxyacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL2 and glycolic acid. LC-MS: R_(t)=0.88; ES+: 654.36

Example 583(1S,5R)-3-((3R)-3-Hydroxybutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide

Synthesized according to typical procedures G and E from bicyclononeneAL2 and (3R)-3-hydroxybutyric acid. LC-MS: R_(t)=0.88; ES+: 682.40.

Example 584 1:1-Mixture of(rac.)-(1R*,5S*)-3-((1R*,2S*)-2-hydroxycyclopentane-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt and(rac.)-(1R*,5S*)-3-((1S*,2R*)-2-hydroxycyclopentanecarbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL2 and cis-2-hydroxy-1-cyclopentane carboxylic acid. LC-MS: R_(t)=0.91;ES+: 708.39.

Example 585(rac.)-(1R*,5S*)-9-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and acetyl chloride. LC-MS: R_(t)=0.92; ES+: 638.34.

Example 586(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-5-oxo-pentanoicacid formate salt

Synthesized according to typical procedures K and E from bicyclononeneBC and glutaric anhydride. LC-MS: R_(t)=0.91; ES+: 710.33.

Example 587(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-5-oxo-pentanoicacid methyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and glutaric acid monomethylester chloride. LC-MS: R_(t)=0.95; ES+:724.33.

Example 588(rac.)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-9-yl)-5-oxo-pentanoicacid ethyl ester formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and glutaric acid monoethylester chloride. LC-MS: R_(t)=0.97; ES+:738.38.

Example 589(rac.)-4-[((11R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)-amino]butyricacid ethyl ester

Synthesized according to typical procedures A and E from bicyclononeneBC and ethyl 4-isocyanatobutyrate. LC-MS: R_(t)=0.95; ES+: 753.37.

Example 590(rac.)-(1R*,5S*)-3-Formyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide

Synthesized according to typical procedure E from bicyclononene AK2.Obtained as side-product after purification by HPLC. LC-MS: R_(t)=0.89;ES+: 624.36.

Example 591(rac.)-3-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)amino]propionicacid formate salt

Synthesized according to typical procedures M and E from Example 579,then typical procedure E. LC-MS: R_(t)=0.87; ES+: 711.31.

Example 592(rac.)-3-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)amino]propionicacid formate salt

Synthesized according to typical procedures G, M and E frombicyclononene BC and ethyl 4-isocyanatopropionate. LC-MS: R_(t)=0.88;ES+: 711.33.

Example 593(rac.)-4-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)amino/butyricacid formate salt

Synthesized according to typical procedures M and E from Example 580.LC-MS: R_(t)=0.89; ES+: 725.35.

Example 594(rac.)-(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,6-Trifluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,3,6-trifluorophenol. LC-MS: R_(t)=0.89; ES+: 624.37.

Example 595(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,3-dimethylphenol. LC-MS: R_(t)=0.91; ES+: 598.42.

Example 596(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,5-dimethylphenol. LC-MS: R_(t)=0.91; ES+: 598.43.

Example 597(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneBB2 and 2-chloro-4,5-dimethylphenol. LC-MS: R_(t)=0.93; ES+: 632.39.

Example 598(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,4-dichlorophenol. LC-MS: R_(t)=0.91; ES+: 640.32.

Example 599(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,3-dichlorophenol. LC-MS: R_(t)=0.91; ES+: 640.34.

Example 600(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,6-difluorophenol. LC-MS: R_(t)=0.88; ES+: 606.39.

Example 601(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,5-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,5-difluorophenol. LC-MS: R_(t)=0.88; ES+: 606.40.

Example 602(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,5-dichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 3,5-dichlorophenol. LC-MS: R_(t)=0.93; ES+: 638.32.

Example 603(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2-chloro-5-methylphenol. LC-MS: R_(t)=0.91; ES+: 618.40.

Example 604(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2-chloro-5-fluorophenol. LC-MS: R_(t)=0.89; ES+: 622.33.

Example 605(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3,6-trichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB2 and 2,5,6-trichlorophenol. LC-MS: R_(t)=0.93; ES+: 674.27.

Example 606(rac.)-(1R*,5S*)-9-(4-Carbamoylbutyryl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneBC and 4-carbamoylbutyric acid. LC-MS: R_(t)=0.88; ES+: 709.39.

Example 607(rac.)-(1R*,5S*)-9-(3-Carbamoylpropionyl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneBC and succinamic acid. LC-MS: R_(t)=0.88; ES+: 695.36.

Example 608(rac.)-(1R*,5S*)-9-(2-Hydroxyaeetyl)-7-{4-[2-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneBC and glycolic acid. LC-MS: R_(t)=0.90; ES+: 654.37.

Example 609(1R,5S)-9-((3S)-3-Hydroxybutyryl)-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneBC and (3R)-3-hydroxybutyric acid. LC-MS: R_(t)=0.91; ES+: 682.41.

Example 610(rac.)-(1R*,5S*)-9-Methanesulfonyl-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and methylsulfonyl chloride. LC-MS: R_(t)=0.95; ES+: 674.38.

Example 611(rac.)-(1R*,5S*)-9-Ethanesulfonyl-7-{4-[2-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures A and E from bicyclononeneBC and ethylsulfonyl chloride. LC-MS: R_(t)=0.97; ES+: 688.37.

Example 612(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2-fluoro-5-methoxybenzyl)amine. LC-MS: R_(t)=0.89;ES+: 652.31.

Example 613(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(3-methoxybenzyl)amine. LC-MS: R_(t)=0.88; ES+:634.34.

Example 614(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2-methoxybenzyl)amine. LC-MS: R_(t)=0.89; ES+:634.32.

Example 615(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,4-dimethoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(3,4-dimethoxybenzyl)amine. LC-MS: R_(t)=0.86; ES+:664.34.

Example 616(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethyl-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.94; ES+: 706.20.

Example 617(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzo[1,3]dioxol-5-ylmethyl-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine. LC-MS:R_(t)=0.91; ES+: 682.28.

Example 618(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(5-fluoro-2-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2-methoxy-5-fluorobenzyl)amine. LC-MS: R_(t)=0.90;ES+: 652.32.

Example 619(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-6-fluorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2-chloro-6-fluorobenzyl)amine. LC-MS: R_(t)=0.89;ES+: 656.30.

Example 620(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2-bromobenzyl)amine. LC-MS: R_(t)=0.91; ES+: 684.23.

Example 621(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,6-difluoro-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2,6-difluorobenzyl)amine. LC-MS: R_(t)=0.88; ES+:640.29.

Example 622(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethyl-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.92; ES+:632.35.

Example 623(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-fluoro-2-methylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2-methyl-3-fluorobenzyl)amine. LC-MS: R_(t)=0.91;ES+: 636.31.

Example 624(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-difluoro-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(3,5-difluorobenzyl)amine. LC-MS: R_(t)=0.93; ES+:672.23.

Example 625(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3,6-difluorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2-chloro-3,6-difluorobenzyl)amine. LC-MS:R_(t)=0.90; ES+: 674.25.

Example 626(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichloro-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2,3-dichlorobenzyl)amine. LC-MS: R_(t)=0.93; ES+:672.25.

Example 627(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoro-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(3-trifluoromethoxybenzyl)amine. LC-MS: R_(t)=0.93;ES+: 688.28.

Example 628(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methylbenzyl)-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(3-methylbenzyl)amine. LC-MS: R_(t)=0.90; ES+:618.36.

Example 629(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-difluoro-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(2,3-difluorobenzyl)amine. LC-MS: R_(t)=0.90; ES+:640.29.

Example 630(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(3-chlorobenzyl)amine. LC-MS: R_(t)=0.91; ES+:638.27.

Example 631(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(4-fluorobenzyl)-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and cyclopropyl(4-fluorobenzyl)amine. LC-MS: R_(t)=0.89; ES+:622.34.

Example 632(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide

Synthesized according to typical procedures H and E from bicyclononeneAJ1 and (2-chlorobenzyl)cyclopropylamine. The title compound waspurified by FC. LC-MS: R_(t)=4.17; ES+: 666.07.

Example 633(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneT2 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.92; ES+: 617.94.

Example 634(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-methoxyphenoxy)ethyl]-methylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneT2 and cyclopropyl-[2-(4-methoxyphenoxy)ethyl]amine. LC-MS: R_(t)=0.84;ES+: 618.03.

Example 635(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl-(3-trifluoromethyl-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneT2 and cyclopropyl-(3-trifluoromethylbenzyl)amine. LC-MS: R_(t)=0.89;ES+: 626.06.

Example 636(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(3,4-dimethylphenoxy)-ethyl]methylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneT2 and cyclopropyl-[2-(3,4-dimethylphenoxy)ethyl]amine. LC-MS:R_(t)=0.91; ES+: 616.13.

Example 637(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3,5-dimethoxybenzyl)methyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneT2 and cyclopropyl-(3,5-dimethoxybenzyl)amine. LC-MS: R_(t)=0.84; ES+:618.11.

Example 638(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ2 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=1.00; ES+:638.14.

Example 639(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(3-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneAJ3 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.99; ES+:638.14.

Example 640(rac.)-(1R*,5S*)-5-[7-{4-[2-(2-Bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxo-pentanoicacid trifluoroacetate salt

Synthesized according to typical procedures K and E from bicyclononeneAL1 and 3,3-dimethyldihydropyran-2,6-dione. LC-MS: R_(t)=0.95; ES+:710.13.

Example 641(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)isopropyl-amide trifluoroacetate salt

Synthesized according to typical procedures H and E from bicyclononeneT2 and (2-chlorobenzyl)isopropylamine. LC-MS: R_(t)=1.03; ES+: 620.20.

Example 642(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,3,6-trichlorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide trifluoroacetate salt

Synthesized according to typical procedures F and E from bicyclononeneU2 and 2,3,6-trichlorophenol. LC-MS: R_(t)=1.00; ES+: 625.99.

Example 643(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneT2 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.89; ES+: 606.07.

Example 644(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(3,4-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU4 and 3,4-dichlorophenol. LC-MS: R_(t)=0.86; ES+: 608.01.

Example 645(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethyl-amide formate salt

Synthesized according to typical procedures F and E from bicyclononeneU4 and 2-chloro-4,5-dimethylphenol. LC-MS: R_(t)=0.87; ES+: 602.07.

Example 646(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)methylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneT2 and (2-chlorobenzyl)methylamine. LC-MS: R_(t)=0.87; ES+: 591.99.

Example 647(rac.)-(1R*,5S*)-3-Methyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

A mixture of bicyclononene AL2 (1 eq.), DIPEA (3 eq.) and methyl iodide(10 eq.) in CH₂Cl₂ was stirred at rt overnight. The solvents wereremoved under reduced pressure and the residue treated according totypical procedure E. LC-MS: R_(t)=0.89; ES+: 610.32.

Example 648(rac.)-(1R*,5S*)-3-Ethyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

A mixture of bicyclononene AL2 (1 eq.), DIPEA (3 eq.) and ethyl iodide(10 eq.) in CH₂Cl₂ was stirred at rt overnight. The solvents wereremoved under reduced pressure and the residue treated according totypical procedure E. LC-MS: R_(t)=0.91; ES+: 624.33.

Example 649(rac.)-(1R*,5S*)-3-(2-Aminoacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures G, L and E frombicyclononene AL2 and Boc-glycine. LC-MS: R_(t)=0.80; ES+: 653.32.

Example 650(rac.)-(1R*,5S*)-3-(3-Aminopropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G, L and E frombicyclononene AL2 and Boc-β-alanine. LC-MS: R_(t)=0.80; ES+: 667.32.

Example 651(rac.)-(1R*,5S*)-3-(5-Morpholin-4-yl-5-oxopentanoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedure H, from bicyclononene AL2 andglutaric anhydride, then according to typical procedure K and E frommorpholine. LC-MS: R_(t)=0.89; ES+: 779.31.

Example 652(rac.)-(1R*,5S*)-3-(2-Tetrazol-1-ylacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G and E from bicyclononeneAL2 and (5H-tetrazol-5-yl)acetic acid. LC-MS: R_(t)=0.91; ES+: 706.23.

Example 653(rac.)-(1R*,5S*)-3-(5-Oxo-5-piperazin-1-ylpentanoyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedure H, from bicyclononene AL2 andglutaric anhydride, then according to typical procedure K, L and E fromBoc-piperazine. LC-MS: R_(t)=0.78; ES+: 778.37.

Example 654 1:1-Mixture of(1R,5S)-3-((2S)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt and(1S,5R)-3-((2S)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures G, L and E frombicyclononene AL2 and Boc-serine. LC-MS: R_(t)=0.79; ES+: 683.34.

Example 655 1:1-Mixture of(1R,5S)-3-((2S)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluoro-phenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt and(1S,5R)-3-((2S)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures G, L and E frombicyclononene AL2 and Boc-alanine. LC-MS: R_(t)=0.80; ES+: 667.32.

Example 656(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and (2,3-dichlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.96; ES+:702.09.

Example 657(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.94; ES+:662.27.

Example 658(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethyl-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.96; ES+: 736.08.

Example 659(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and (2-bromobenzyl)cyclopropylamine. LC-MS: R_(t)=0.92; ES+: 682.20.

Example 660(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.93; ES+:668.20.

Example 661(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-ethylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.93; ES+: 656.20.

Example 662(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (6-chlorobenzo-[1,3]dioxol-5-ylmethyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine. LC-MS:R_(t)=0.93; ES+: 712.15.

Example 663(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(3,5-dimethoxybenzyl)amine. LC-MS: R_(t)=0.92; ES+:694.20.

Example 664(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(3-methoxybenzyl)amine. LC-MS: R_(t)=0.91; ES+:664.25.

Example 665(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichloro-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: R_(t)=0.92; ES+:672.22.

Example 666(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoro-methylbenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.93; ES+: 706.09.

Example 667(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and (3-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.93; ES+:668.21.

Example 668(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(3-methylbenzyl)amine. LC-MS: R_(t)=0.93; ES+:648.23.

Example 669(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(2-fluoro-5-methoxybenzyl)amine. LC-MS: R_(t)=0.92;ES+: 682.20.

Example 670(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)-ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: R_(t)=0.95.; ES+:684.20.

Example 671(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2-chloro-3,6-difluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB1 and 2-chloro-3,6-difluorophenol. LC-MS: R_(t)=0.93.; ES+: 654.28.

Example 672(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethylbenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.96; ES+: 716.18.

Example 673(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,4-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(3,4-dimethoxybenzyl)amine. LC-MS: R_(t)=0.89; ES+:694.23.

Example 674(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(3-trifluoromethoxybenzyl)amine. LC-MS: R_(t)=0.95;ES+: 718.13.

Example 675(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoro-methylbenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.97; ES+: 758.08.

Example 676(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: R_(t)=0.96; ES+:724.02.

Example 677(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethyl-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and cyclopropyl-(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.92; ES+:648.25.

Example 678(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and cyclopropyl(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.95; ES+:684.12.

Example 679(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.94; ES+:642.31.

Example 680(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: R_(t)=0.92; ES+:718.05.

Example 681(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and (2-bromobenzyl)cyclopropylamine. LC-MS: R_(t)=0.94; ES+: 694.15.

Example 682(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: R_(t)=0.93; ES+:690.06.

Example 683(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and cyclopropyl-(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.91; ES+:632.31.

Example 684(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.94; ES+:690.07.

Example 685(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoro-methylbenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.93; ES+: 752.06.

Example 686(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and (2-bromobenzyl)cyclopropylamine. LC-MS: R_(t)=0.95; ES+: 733.99.

Example 687(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethyl-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and cyclopropyl-(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.91; ES+:678.22.

Example 688(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethyl-benzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.94; ES+: 724.13.

Example 689(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and (3-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.93; ES+:648.26.

Example 690(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.94; ES+: 678.12.

Example 691(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and (2-bromobenzyl)cyclopropylamine. LC-MS: R_(t)=0.90; ES+:684.11.

Example 692(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and cyclopropyl-(2,3-dichlorobenzyl)amine. LC-MS: R_(t)=0.94; ES+:670.17

Example 693(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(3-methoxybenzyl)amine. LC-MS: R_(t)=0.91; ES+:644.32.

Example 694(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and cyclopropyl(2-bromobenzyl)amine. LC-MS: R_(t)=0.91; ES+: 728.04.

Example 695(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and cyclopropyl(2,3-dimethylbenzyl)amine. LC-MS: R_(t)=0.93; ES+:628.30.

Example 696(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and cyclopropyl-(3-methoxybenzyl)amine. LC-MS: R_(t)=0.92; ES+:686.14.

Example 697(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(2-fluoro-5-methoxybenzyl)amine. LC-MS: R_(t)=0.91;ES+: 662.29.

Example 698(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and (2-bromobenzyl)cyclopropylamine. LC-MS: R_(t)=0.93; ES+: 680.15.

Example 699(rac.)-(1R*5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.90; ES+:638.22.

Example 700(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and cyclopropyl-(3,5-dimethoxybenzyl)amine. LC-MS: R_(t)=0.93; ES+:716.14.

Example 701(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and (2-bromobenzyl)cyclopropylamine. LC-MS: R_(t)=0.91; ES+: 700.07.

Example 702(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (6-chloro-benzo[1,3]dioxol-5-ylmethyl)-cyclopropylamide formatesalt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine. LC-MS:R_(t)=0.93; ES+: 694.17.

Example 703(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.91; ES+:656.19.

Example 704(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethylbenzyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and (2-chloro-3-trifluoromethylbenzyl)cyclopropylamine. LC-MS:R_(t)=0.95; ES+: 702.17.

Example 705(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(3-methylbenzyl)amine. LC-MS: R_(t)=0.92; ES+:628.32.

Example 706(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.90; ES+: 642.19.

Example 707(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and cyclopropyl-(2-fluoro-5-methoxybenzyl)amine. LC-MS: R_(t)=0.88;ES+: 652.26.

Example 708(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and cyclopropyl(2-chlorobenzyl)amine. LC-MS: R_(t)=0.92; ES+:634.22.

Example 709(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and cyclopropyl-(3,5-dimethoxybenzyl)amine. LC-MS: R_(t)=0.88; ES+:708.14.

Example 710(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and cyclopropyl-(3-methoxybenzyl)amine. LC-MS: R_(t)=0.87; ES+:634.27.

Example 711(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and (3-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.94; ES+:690.09.

Example 712(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy-ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-difluorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN4 and cyclopropyl-(3,5-difluorobenzyl)amine. LC-MS: R_(t)=0.93; ES+:670.22.

Example 713(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and cyclopropyl-(2-fluoro-5-methoxybenzyl)amine. LC-MS: R_(t)=0.93;ES+: 702.40.

Example 714(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,4-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and cyclopropyl-(3,4-dimethoxybenzyl)amine. LC-MS: R_(t)=0.90; ES+:716.10.

Example 715(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (6-chloro-benzo[1,3]-dioxol-5-ylmethyl)cyclopropylamide formatesalt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine. LC-MS:R_(t)=0.90; ES+: 684.19.

Example 716(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and (3-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.90; ES+:682.16.

Example 717(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,4-dimethoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and cyclopropyl-(3,4-dimethoxybenzyl)amine. LC-MS: R_(t)=0.97; ES+:758.08.

Example 718(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-ethylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.89; ES+: 626.25.

Example 719(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and cyclopropyl-(3,5-dimethoxybenzyl)amine. LC-MS: R_(t)=0.90; ES+:660.29.

Example 720(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methyl-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and cyclopropyl-(3-methylbenzyl)amine. LC-MS: R_(t)=0.94; ES+:670.22.

Example 721(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and cyclopropyl-(2-fluoro-5-methoxybenzyl)amine. LC-MS: R_(t)=0.89;ES+: 668.25.

Example 722(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-difluorobenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(3,5-difluorobenzyl)amine. LC-MS: R_(t)=0.92; ES+:650.23.

Example 723(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and cyclopropyl-(3,5-dimethoxybenzyl)amine. LC-MS: R_(t)=0.89; ES+:680.22.

Example 724(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and cyclopropyl(3-chlorobenzyl)amine. LC-MS: R_(t)=0.90; ES+:638.22.

Example 725(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and (2-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.90; ES+:684.12.

Example 726(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,4-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(3,4-dimethoxybenzyl)amine. LC-MS: R_(t)=0.88; ES+:674.31.

Example 727(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN3 and cyclopropyl-(3-trifluoromethoxybenzyl)amine. LC-MS: R_(t)=0.95;ES+: 698.22.

Example 728(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and cyclopropyl-(3-methylbenzyl)amine. LC-MS: R_(t)=0.89; ES+:618.28.

Example 729(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-chloro-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN10 and cyclopropyl-(3,5-dimethoxybenzyl)amine. LC-MS: R_(t)=0.88; ES+:664.27.

Example 730(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methyl-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and cyclopropyl-(3-methylbenzyl)amine. LC-MS: R_(t)=0.90; ES+:634.21.

Example 731(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and cyclopropyl-(2-fluoro-5-methoxybenzyl)amine. LC-MS: R_(t)=0.89;ES+: 696.14.

Example 732(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.90; ES+: 672.14.

Example 733(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine. LC-MS:R_(t)=0.91; ES+: 700.12.

Example 734(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)cyclopropyl-amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN5 and (3-chlorobenzyl)cyclopropylamine. LC-MS: R_(t)=0.91; ES+:656.19.

Example 735(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (6-chloro-benzo[1,3]dioxol-5-ylmethyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine. LC-MS:R_(t)=0.92; ES+: 678.20.

Example 736(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxy-benzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN2 and cyclopropyl-(3-methoxybenzyl)amine. LC-MS: R_(t)=0.88; ES+:678.20.

Example 737(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-ethylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and (2-chlorobenzyl)ethylamine. LC-MS: R_(t)=0.91; ES+: 622.26.

Example 738(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(4-chloro-2-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methylbenzyl)amide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN7 and cyclopropyl-(3-methylbenzyl)amine. LC-MS: R_(t)=0.91; ES+:614.32.

Example 739(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamide formate salt

Synthesized according to typical procedures H and E from bicyclononeneBN9 and (6-chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine. LC-MS:R_(t)=0.94; ES+: 734.06.

Example 740(rac.)-(1R,5S)-7-{4-[3-(2,3,6-Trifluorophenoxy)propylphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide

From Example 149, separated by chiral preparative HPLC.

Example 741(rac.)-(1S,5R)-7-{4-[3-(2,3,6-Trifluorophenoxy)propylphenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide

From Example 149, separated by chiral preparative HPLC.

Example 742(rac.)-(1R*,5S*)-3-Acetyl-7-{4-[3-(2,6-dichloro-4-methylphenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)-cyclopropylamide formate salt

Synthesized according to typical procedures F and E from bicyclononeneBB1 and 2,6-dichloro-4-methylphenol. LC-MS: R_(t)=0.96; ES+: 666.35.

Example 743(rac.)-(1R*,5S*)-7-{4-[3-(2-Bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropyl-amide

Synthesized according to typical procedure E from bicyclononene AL20.LC-MS: R_(t)=0.86; ES+: 640.21.

The following assay was carried out in order to determine the activityof the compounds of general formula I and their salts.

Inhibition of Human Recombinant Renin by the Compounds of the Invention

The enzymatic in vitro assay was performed in 384-well polypropyleneplates (Nunc). The assay buffer consisted of 10 mM PBS (Gibco BRL)including 1 mM EDTA and 0.1% BSA. The incubates were composed of 50 μLper well of an enzyme mix and 2.5 μL of renin inhibitors in DMSO. Theenzyme mix was premixed at 4° C. and consists of the followingcomponents:

-   -   human recombinant renin (0.16 ng/mL)•synthetic human        angiotensin(1-14) (0.5    -   hydroxyquinoline sulfate (1 mM)

The mixtures were then incubated at 37° C. for 3 h. To determine theenzymatic activity and its inhibition, the accumulated Ang I wasdetected by an enzyme immunoassay (EIA) in 384-well plates (Nunc). 5 μLof the incubates or standards were transferred to immuno plates whichwere previously coated with a covalent complex of Ang I and bovine serumalbumin (Ang I —BSA). 75 μL of Ang I-antibodies in essay buffer aboveincluding 0.01% Tween 20 were added and a primary incubation made at 4°C. overnight. The plates were washed 3 times with PBS including 0.01%Tween 20, and then incubated for 2 h at rt with an antirabbit-peroxidasecoupled antibody (WA 934, Amersham). After washing the plates 3 times,the peroxidase substrate ABTS(2.2′-azino-di-(3-ethyl-benzthiazolinsulfonate), was added and theplates incubated for 60 min at room temperature. After stopping thereaction with 0.1 M citric acid pH 4.3 the plate was evaluated in amicroplate reader at 405 nm. The percentage of inhibition was calculatedof each concentration point and the concentration of renin inhibitionwas determined that inhibited the enzyme activity by 50% (IC₅₀). TheIC₅₀-values of all compounds tested are below 100 nM. However selectedcompounds exhibit a very good bioavailability and are metabolically morestable than prior art compounds.

1-18. (canceled)
 19. A method for treating or preventing a diseaseassociated with dysregulation of the renin-angiotensin system (RAS),comprising administering a compound of general formula I

wherein X and W represent a —CH— group; V represents —(CH₂)_(r)—;-A-(CH₂)_(s)—; —CH₂-A-(CH₂)_(t)—; —(CH₂)_(s)-A-; —(CH₂)₂-A-(CH₂)_(u)—;-A-(CH₂)_(v)—B—; —CH₂—CH₂—CH₂-A-CH₂—; -A-CH₂—CH₂—B—CH₂—;—CH₂-A-CH₂—CH₂—B—; —CH₂—CH₂—CH₂-A-CH₂—CH₂—; —CH₂—CH₂—CH₂—CH₂-A-CH₂—;-A-CH₂—CH₂—B—CH₂—CH₂—; —CH₂-A-CH₂—CH₂—B—CH₂—; —CH₂-A-CH₂—CH₂—CH₂—B—; or—CH₂—CH₂-A-CH₂—CH₂—B—; A and B independently represent —O—; —S—; —SO—;or —SO₂—; U represents aryl; or heteroaryl; T represents —CONR¹—;—(CH₂)_(p)OCO—; —(CH₂)_(p)N(R¹)CO—; —(CH₂)_(p)N(R¹)SO₂—; or —COO—; Qrepresents lower alkylene; or lower alkenylene; M represents hydrogen;cycloalkyl; aryl; heterocyclyl; or heteroaryl; L represents —R³; —COR³;—COOR³; —CONR²R³; —SO₂R³; —SO₂NR²R³; or —COCH (Aryl)₂; R¹ representshydrogen; lower alkyl; lower alkenyl; lower alkinyl; cycloalkyl; aryl;or cycloalkyl-lower alkyl; R² and R², independently represent hydrogen;lower alkyl; lower alkenyl; cycloalkyl; or cycloalkyl-lower alkyl; R³represents hydrogen; lower alkyl; lower alkenyl; cycloalkyl; aryl;heteroaryl; heterocyclyl; cycloalkyl-lower alkyl; aryl-lower alkyl;heteroaryl-lower alkyl; heterocyclyl-lower alkyl; aryloxy-lower alkyl;or heteroaryloxy-lower alkyl; wherein these groups may be unsubstitutedor mono-, di- or tri-substituted with hydroxy, —OCOR², —COOR², loweralkoxy, cyano, —CONR²R², —CO-morpholin-4-yl, —CO-((4-loweralkyl)piperazin-1-yl), —NH(NH)NH², —NR⁴R⁴, or lower alkyl, with theproviso that a carbon atom is attached at the most to one heteroatom incase this carbon atom is sp3-hybridized; R⁴ and R^(4′) independentlyrepresent hydrogen; lower alkyl; cycloalkyl; cycloalkyl-lower alkyl;hydroxyl-lower alkyl; —COOR²; or —CONH₂; m represents the integer 1 andn represents the integer 0; p is the integer 1, 2, 3 or 4; r is theinteger 3, 4, 5, or 6; s is the integer 2, 3, 4, or 5; t is the integer1, 2, 3, or 4; u is the integer 1, 2, or 3; and v is the integer 2, 3,or 4; or optically pure enantiomers, mixtures of enantiomers,diastereomers, mixtures of diastereomers, diastereomeric racemates,mixtures of diastereomeric racemates, or the meso-form; orpharmaceutically acceptable salts of said compound.
 20. The method ofclaim 19, comprising administering the compound of general formula I,wherein L represents —COR^(3″); —COOR^(3″); or —CONR^(2″)R^(3″); andR^(2″) and R^(3″) represent independently lower alkyl or lowercycloalkyl-lower alkyl, which lower alkyl and lower cycloalkyl-loweralkyl are unsubstituted or mono-substituted with halogen, —CN, —OH,—OCOCH₃, —CONH₂, —COOH, or —NH₂, with the proviso that a carbon atom isattached at the most to one heteroatom in case this carbon atom issp3-hybridized.
 21. The method of claim 19, comprising administering thecompound of general formula I, wherein T represents —CONR¹; Q representsmethylene; and M represents hydrogen; aryl; or heteroaryl.
 22. Themethod of claim 19, comprising administering the compound of generalformula I, wherein V represents —CH₂CH₂O—; —CH₂CH₂CH₂O—; or —OCH₂CH₂O—.23. The method of claim 19, comprising administering the compound ofgeneral formula I, wherein U is a mono-, di-, or tri-substituted phenyl,wherein the substituents are halogen, lower alkyl or lower alkoxy. 24.The method of claim 19, wherein said disease is selected from the groupconsisting of hypertension, congestive heart failure, pulmonaryhypertension, cardiac insufficiency, renal insufficiency, renal ormyocardial ischemia, atherosclerosis, renal failure, erectiledysfunction, glomerulonephritis, renal colic, glaucoma, diabeticcomplications, complications after vascular or cardiac surgery,restenosis, and complications of treatment with immunosuppressive agentsafter organ transplantation.
 25. A method of treating or preventing adisease associated with dysregulation of the RAS, comprisingadministering to a subject a compound selected from the group consistingof: (2-methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-(2-thiophen-2-ylacetyl)-3,9-diazabicyclo[3.3.1]non-6-en-6-yl-methylester; (2-methoxyphenyl)acetic acid(1R*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-yl-methylester; (2-methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-(quinoxaline-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-en-6-yl-methylester;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-chlorophenyl)ethyl]methyl-amide; (2-methoxyphenyl)acetic acid(1R*,5S*)-3-(benzo[b]thiophene-3-carbonyl)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-6-yl-methylester; (2-methoxyphenyl)acetic acid(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxy-benzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester; (2-methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-phenylmethanesulfonyl-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(4-methoxyphenyl)ethyl]-methylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid[2-(4-chlorophenyl)ethyl]methylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid[2-(3-chlorophenyl)ethyl]methylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid ethylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid[2-(3-methoxyphenyl)ethyl]methylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide; (2-methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3-methyl-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(3,4-dimethoxyphenyl)ethyl]methylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,5-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;N-(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide; (2-methoxyphenyl)acetic acid(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)-propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethylester;N-((1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-6-ylmethyl)-2-(2-methoxyphenyl)-N-methyl-acetamide;N-(1R*,5S*)-3-acetyl-7-{4-[2-(2-tert-butyl-4-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,5-difluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methyl(3-phenylpropyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-acetylphenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid [2-(2-methoxyphenyl)ethyl]methylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylmethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,5-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-[4-(2-o-tolyloxyethyl)phenyl]-3,9-diazabicyclo-[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(3-isopropylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid methylphenethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-5-[7-{4-[2-(2-bromo-5-fluorophenoxy)ethyl]phenyl}-6-(methylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxo-pentanoicacid;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxo-pentanoicacid;5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxo-pentanoicacid methyl ester;(1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzylcyclopropylamide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)amide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluorobenzyl)amide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethylbenzyl)amide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-methylbenzyl)amide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-phenethylamide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid[2-(2-chlorophenyl)ethyl]cyclopropylamide;(1R*,5S*)-3-(4-carbamoylbutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide;(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropyl-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo-[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R,5S)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-{cyclopropyl[2-(4-methoxyphenoxy)ethyl]-carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-{cyclopropyl-[2-(4-methoxyphenoxy)ethyl]carbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(2-m-tolyloxyethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(2-m-tolyloxyethyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3R*)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(3S*)-5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-3-hydroxy-5-oxopentanoicacid;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl(3,5-dimethoxybenzyl)amide;5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl(3-trifluoromethylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl(2-p-tolylethyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester;5-((1R,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester;5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester;5-(1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)-carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid;(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,3-dihydroxy-4-oxobutyricacid;5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{cyclopropyl-[2-(3-methylphenoxy)ethyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-5-oxopentanoicacid;5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2,3-difluorophenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(2-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid methyl ester;5-{(1R*,5S)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxo-pentanoicacid;5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxo-pentanoicacid;5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-(cyclopropylphenethylcarbamoyl)-3,9-diazabicyclo[3.3.1]non-6-en-3-yl]-2,2-dimethyl-5-oxopentanoicacid;5-((1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-{[2-(4-methylphenyl)ethyl]cyclopropylcarbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-{(1R*,5S)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid;(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid;(2S*,3R*)-4-{(1R*,5S)-7-{4-[3-(2-bromo-5-fluoro-phenoxy)propyl]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,3-dihydroxy-4-oxobutyricacid;5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[(3-trifluoromethylbenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S)-6-[(2-methylbenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R,5S*)-6-[(2-chlorobenzyl)ethycarbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid;5-{(1R*,5S*)-4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;5-((1R*,5S*)-6-(benzylcyclopropylcarbamoyl)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid methyl ester;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-methylbenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-5-oxopentanoicacid;5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-((1R*,5S*)-6-[(2-chlorobenzyl)ethylcarbamoyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl-(2-fluorobenzyl)carbamoyl]-3,9-diazabicyclo[3.3.1]non-6-en-3-yl}-2,2-dimethyl-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl-(3,5-dimethoxybenzyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-[cyclopropyl-(2-p-tolylethyl)carbamoyl]-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl-[2-(2-hydroxyethyl)benzyl]carbamoyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid;5-((1R*,5S*)-6-(cyclopropylphenethylcarbamoyl)-7-{4-[2-(2,3,5-trimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-2,2-dimethyl-5-oxopentanoicacid;(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide;(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-[(2-chlorobenzyl)cyclopropylamide]3-dimethylamide;(1R*,5S*)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylicacid 6-[(2-chlorobenzyl)cyclopropylamide]3-diethylamide;(1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic acid methylester;(1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylicacid ethyl ester;(1R*,5S*)-3-methanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-ethanesulfonyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;5-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-5-oxopentanoicacid ethyl ester;4-((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-en-3-yl)-4-oxobutyricacid;3-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)-amino]propionicacid ethyl ester;4-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)amino]butyricacid ethyl ester;(1R*,5S*)-3-(3-carbamoylpropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-(2-hydroxyacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1S,5R)-3-((3R)-3-hydroxybutyryl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-((1R*,2S*)-2-hydroxycyclopentanecarbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-((1S*,2R*)-2-hydroxycyclopentanecarbonyl)-7-{4-[3-(2,3,6-trifluorophenoxy)-propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-formyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;3-[((1R*,5S*)-6-[(2-chlorobenzyl)cyclopropylcarbamoyl]-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carbonyl)-amino]propionicacid;(1R*,5S*)-3-acetyl-7-{4-[2-(2,3,6-trifluorophenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxy-benzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxybenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,4-dimethoxybenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethylbenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid benzo[1,3]dioxol-5-ylmethyl-cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-6-fluorobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-difluorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethoxy-benzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methylbenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)cyclopropylamide;(1R*,5S*)-7-{4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl}-3-(4-carbamoylbutyryl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide;(1R*,5S*)-3-(5-morpholin-4-yl-5-oxopentanoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-(2-tetrazol-1-ylacetyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-(5-oxo-5-piperazin-1-ylpentanoyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R,5S)-3-((2S)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1S,5R)-3-((2S)-2-amino-3-hydroxypropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R,5S)-3-((2S)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1S,5R)-3-((2S)-2-aminopropionyl)-7-{4-[3-(2,3,6-trifluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethyl-benzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)ethylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (6-chlorobenzo-[1,3]dioxol-5-ylmethyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,5-dimethoxybenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methoxybenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenxoy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenxoy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethylbenzyl)-cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (3-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-methylbenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2-fluoro-5-methoxybenzyl)-amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethylbenzyl)-cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3,4-dimethoxybenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(3-trifluoromethoxybenzyl)-amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chloro-3-trifluoromethylbenzyl)-cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-fluorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-bromobenzyl)cyclopropylamide;(1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dichlorobenzyl)amide;(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-fluorophenxoy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid cyclopropyl-(2,3-dimethylbenzyl)amide;(1R,5S)-7-{4-[3-(2,3,6-trifluorophenxoy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide; and(1S,5R)-7-{4-[3-(2,3,6-trifluorophenxoy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylicacid (2-chlorobenzyl)cyclopropylamide.
 26. The method of claim 25,wherein said disease is selected from the group consisting ofhypertension, congestive heart failure, pulmonary hypertension, cardiacinsufficiency, renal insufficiency, renal or myocardial ischemia,atherosclerosis, renal failure, erectile dysfunction,glomerulonephritis, renal colic, glaucoma, diabetic complications,complications after vascular or cardiac surgery, restenosis, andcomplications of treatment with immunosuppressive agents after organtransplantation.